Immunology/Inflammation - MedchemExpress.com · Immunology/Inflammation ... Besides resolving infection and injury, chronic inflammation is a risk factor for cancer. Immunity has

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Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Immunology/Inflammation

The immune system has evolved to survey and respond appropriately to the universe of foreign pathogens, deploying anintricate repertoire of mechanisms that keep responses to host tissues in check. The immune system is typically dividedinto two categories--innate and adaptive. Innate immunity refers to nonspecific defense mechanisms that come into playimmediately or within hours of an antigen's appearance in the body. Adaptive immunity refers to antigen-specificimmune response. The antigen first must be processed and recognized, and then the adaptive immune system creates anarmy of immune cells specifically designed to attack that antigen. For the adaptive immune system, specificity andsensitivity are provided by a large repertoire of antigen T-cell receptors (TCRs) constructed in their extracellular domain torecognize antigenic peptide fragments restricted and presented by histocompatibility complex molecules, and coupledthrough intracellular domains to signal transduction modules that serve to transmit environmental cues inside the cell.Inflammation is triggered when innate immune cells detect infection or tissue injury. Pattern recognition receptors (PRRs)respond to pathogen-associated molecular patterns (PAMPs) or host-derived damage-associated molecular patterns(DAMPs) by triggering activation of NF-κB, AP1, CREB, c/EBP, and IRF transcription factors. Induction of genes encodingenzymes, chemokines, cytokines, adhesion molecules, and regulators of the extracellular matrix promotes the recruitmentand activation of leukocytes. Besides resolving infection and injury, chronic inflammation is a risk factor for cancer.Immunity has a major impact on inflammatory diseases and cancer, and biologics targeting immune cells and theirfactors. Immunosuppressant drugs suppress, or reduce, the strength of the body’s immune system, and have been used inthe treatment of organ transplantation or autoimmunine diseases. Immunomodulator drugs have contributed to thesignificant improvement against cancer and other related diseases. References:[1] Sakaguchi S, et al. Immunol Cell Biol. 2012 Mar;90(3):277-87. doi: 10.1038/icb.2012.4.[2] Newton K, et al. Cold Spring Harb Perspect Biol. 2012 Mar; 4(3): a006049.

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2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]


• STING 99

• Thrombopoietin Receptor 102

• Toll-like Receptor (TLR) 104

• Arginase 3

• Aryl Hydrocarbon Receptor 6

• CCR 9

• CD73 14

• Complement System 16

• COX 19

• CXCR 32

• FKBP 37

• FLAP 39

• Galectin 41

• Histamine Receptor 43

• IFNAR 57

• Interleukin Related 59

• IRAK 64

• MyD88 67

• NO Synthase 69

• NOD-like Receptor (NLR) 73

• PD-1/PD-L1 76

• PGE synthase 79

• Reactive Oxygen Species 82

• Salt-inducible Kinase (SIK) 95

• SPHK 97

Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Target List in Immunology/Inflammation

https://www.MedChemExpress.com

Arginase

Arginase, an enzyme within the urea cycle in the liver, is also found inmany other cells and tissues, including the lung. Arginase is present in2 isoforms: arginase I, the hepatic isoform; and arginase II, theextrahepatic isoform; each of which is encoded by a distinct gene.The expression and function of arginase I in macrophages,hepatocytes, and vascular smooth muscle cells, is stimulated bylipopolysaccharide (LPS), IL-13, altered oxygen tension, and balloondilatation of coronary arteries. The activation and expression ofendothelial arginase II can also be induced by a variety of vascularinsults.Arginase competitively inhibits nitric oxide synthase (NOS) via use of

the common substrate L-arginine. Inhibition of arginase activity enhances a variety of parameters relevant to allergicairways disease, possibly by altering NO homeostasis. Arginase inhibition actively augments NO production and hasbeneficial effects on normal cardiac function and on vascular dysfunction typical of atherogenesis, aging, and erectiledysfunction, and sickle cell disease.


https://www.MedChemExpress.com/Targets/Arginase.html


Purity: 99.0%Clinical Data: No Development ReportedSize: 5 mg

Purity: 99.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg

Purity: 97.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in Water,

5 g

Purity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg

Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg

Purity: 98.0%Clinical Data: Phase 3Size: 10mM x 1mL in Water,

5 mg, 10 mg, 25 mg, 50 mg

Purity: 98.00%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Arginase Inhibitors & Modulators

Bioactivity: Arginase inhibitor 1 is a potent inhibitor of human arginases Iand with s of 223 and 509 nM, respectively.II IC50

Bioactivity: BEC HCl is a slow-binding and competitive Arginase IIinhibitor with Ki of 0.31 μM (ph 7.5). target: Arginase II[1]; In vitro: BEC HCl causes significant enhancement ofNO-dependent smooth muscle relaxation in this tissue. [2] BECHCl enhances perivascular and peribronchiolar lung…

Bioactivity: CB-1158 is a potent and orally bioavailable inhibitor of, with s of 86 and 296 nM for recombinant humanarginase IC50

arginase 1 and 2, respectively.

Bioactivity: CB-1158 Hydrochloride is a potent and orally bioavailableinhibitor of , with s of 86 and 296 nM forarginase IC50recombinant human arginase 1 and 2, respectively.

Bioactivity: DL-Norvaline, a derivative of , L-norvaline is aL-norvalinenon-competitive inhibitor of arginase.

Bioactivity: nor-NOHA acetate is a specific and reversible arginaseinhibitor, induces apoptosis in ARG2-expressing cells underhypoxia but not normoxia. Anti-leukemic activity, effective inendothelial dysfunction, immunosuppression and metabolism

.[1]

Bioactivity: Piceatannol 3'-O-glucoside, an active component of Rhubarb,activates endothelial ( ) throughnitric oxide NO synthaseinhibition of arginase activity with s of 11.22 µM andIC5011.06 µM against and , respectively.arginase I arginase II

Arginase inhibitor 1 Cat. No.: HY-15775

BEC hydrochloride Cat. No.: HY-19548A

CB-1158 (INCB01158) Cat. No.: HY-101979

CB-1158 Hydrochloride (INCB01158 Hydrochloride) Cat. No.: HY-101979A

DL-Norvaline (2-Aminopentanoic acid) Cat. No.: HY-W010510

nor-NOHA acetate (Nω-hydroxy-nor-Arginine acetate) Cat. No.: HY-112885A

Piceatannol 3'-O-glucoside (Quzhaqigan) Cat. No.: HY-N2237

https://www.MedChemExpress.com/Targets/Arginase.htmlhttps://www.MedChemExpress.com/Arginase-inhibitor-1.htmlhttps://www.MedChemExpress.com/BEC-hydrochloride.htmlhttps://www.MedChemExpress.com/CB-1158.htmlhttps://www.MedChemExpress.com/CB-1158_Hydrochloride.htmlhttps://www.MedChemExpress.com/DL-Norvaline.htmlhttps://www.MedChemExpress.com/nor-NOHA_acetate.htmlhttps://www.MedChemExpress.com/Piceatannol_3_acute_-O-glucoside.html

Aryl Hydrocarbon ReceptorAhR

Aryl Hydrocarbon Receptor (AhR or AHR or ahr or ahR) is a proteinthat in humans is encoded by the AHR gene. The aryl hydrocarbonreceptor is a ligand-activated transcription factor involved in theregulation of biological responses to planar aromatic (aryl)hydrocarbons, and regulates xenobiotic-metabolizing enzymes suchas cytochrome P450s, most notably cyp 1A1.Aryl Hydrocarbon Receptor is a member of the family of basichelix-loop-helix transcription factors. AhR binds several exogenousligands including natural plant flavonoids, polyphenolics and indoles,as well as synthetic polycyclic aromatic hydrocarbons and dioxin-likecompounds. AhR is a cytosolic transcription factor that is normally

inactive, binding to several co-chaperones. Upon ligand binding to chemicals such as2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), the chaperones dissociate resulting in AhR translocating into the nucleusand dimerizing with ARNT (AhR nuclear translocator), leading to changes in gene transcription.


https://www.MedChemExpress.com/Targets/Aryl Hydrocarbon Receptor.html



50 mg


5 mg, 10 mg, 50 mg, 100 mg

Purity: 98.0%Clinical Data: Phase 2Size: 10mM x 1mL in DMSO,

200 mg, 1 g

Purity: 99.90%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg


1 mg, 5 mg, 10 mg, 25 mg, 50 mg

Purity: 98.0%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

50 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg



50 mg

Aryl Hydrocarbon Receptor Inhibitors & Modulators

Bioactivity: 1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as anactivator of aryl hydrocarbon receptor ( ).AhR

Bioactivity: AHR antagonist 1 is an aryl hydrocarbon receptor (AHR)antagonist extracted from patent WO2017202816A1, example 23,has an of 39.9 nM in human cell line .IC50

[1]

Bioactivity: CAY 10465 is a selective and high-affinity agonist, withAhRa of 0.2 nM, and shows no effect on estrogen receptor (K Ki i>100000 nM).

Bioactivity: CH-223191 is a potent and specific antagonist of aryl. CH-223191 blocks the binding ofhydrocarbon receptor (AhR)

TCDD to AhR with an of 0.03 µM.IC50

Bioactivity: Diosmin is a flavonoid found in a variety of citrus fruits andalso an agonist of the ( ).aryl hydrocarbon receptor AhR

Bioactivity: FICZ is a potent agonist witharyl hydrocarbon receptor (AhR)a of 70 pM.Kd

Bioactivity: GNF351 is a full antagonist.aryl hydrocarbon receptor (AHR)GNF351 competes with a photoaffinity AHR ligand for binding tothe AHR with an of 62 nM. GNF351 is minimal toxicity inIC50mouse or human keratinocytes .[1]

Bioactivity: Indole-3-carbinol (I3C) inhibits activity and also isNF-κBan ( ) agonist, and an inhibitorAryl hydrocarbon receptor AhRof (WW domain-containing ubiquitin E3 ligase 1).WWP1

Bioactivity: ITE is a potent endogenous agonist of aryl hydrocarbonreceptor ( ), binding directly to , with a of 3 nM.AhR AHR KiITE also has immunosuppressive activity.

Bioactivity: L-Kynurenine is a metabolite of the amino acid L-tryptophan.L-Kynurenine is an agonist.aryl hydrocarbon receptor

1,4-Chrysenequinone (Chrysene-1,4-dione) Cat. No.: HY-111441

AHR antagonist 1 Cat. No.: HY-111449

CAY 10465 Cat. No.: HY-112627

CH-223191 Cat. No.: HY-12684

Diosmin Cat. No.: HY-N0178

FICZ (6-Formylindolo[3,2-b]carbazole) Cat. No.: HY-12451

GNF351 Cat. No.: HY-102023

Indole-3-carbinol (I3C; 3-Indolemethanol) Cat. No.: HY-N0170

ITE Cat. No.: HY-19317

L-Kynurenine Cat. No.: HY-104026

https://www.MedChemExpress.com/Targets/Aryl Hydrocarbon Receptor.htmlhttps://www.MedChemExpress.com/1,4-Chrysenequinone.htmlhttps://www.MedChemExpress.com/ahr-antagonist-1.htmlhttps://www.MedChemExpress.com/CAY_10465.htmlhttps://www.MedChemExpress.com/CH-223191.htmlhttps://www.MedChemExpress.com/Diosmin.htmlhttps://www.MedChemExpress.com/FICZ.htmlhttps://www.MedChemExpress.com/gnf351.htmlhttps://www.MedChemExpress.com/Indole-3-carbinol.htmlhttps://www.MedChemExpress.com/ITE.htmlhttps://www.MedChemExpress.com/L-Kynurenine.html


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10 mg, 50 mg, 100 mg


100 mg


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10 mg, 50 mg, 100 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg

Bioactivity: Mivotilate is a nontoxic, potent activator of the aryl, and acts as a hepatoprotectivehydrocarbon receptor (AhR)

agent.

Bioactivity: PDM2 is a selective, high-affinity aryl hydrocarbon receptor () antagonist with an of 1.2±0.4 nM.AhR Ki

Bioactivity: Pifithrin-α hydrobromide is a inhibitor which blocks itsp53transcriptional activity and prevents cells from apoptosis.Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor

agonist.(AhR)

Bioactivity: Skatole is produced by intestinal bacteria, regulatesintestinal epithelial cellular functions through activating

and .aryl hydrocarbon receptors p38 [1]

Bioactivity: StemRegenin 1 is a potent aryl hydrocarbon receptor ( )AhRantagonist with of 127 nM.IC50

Bioactivity: Tapinarof is a natural ( )aryl hydrocarbon receptor AhRagonist with an of 13 nM.EC50


Mivotilate (YH439) Cat. No.: HY-100242

PDM2 Cat. No.: HY-112629

Pifithrin-α hydrobromide (Pifithrin hydrobromide; PFTα hydrobromide) Cat. No.: HY-15484

Skatole (3-Methylindole; 3-Methyl-1H-indole) Cat. No.: HY-W007355

StemRegenin 1 (SR1) Cat. No.: HY-15001

Tapinarof (WBI 1001; Benvitimod; GSK2894512) Cat. No.: HY-109044

https://www.MedChemExpress.com/Mivotilate.htmlhttps://www.MedChemExpress.com/PDM2.htmlhttps://www.MedChemExpress.com/Pifithrin-_alpha_-hydrobromide.htmlhttps://www.MedChemExpress.com/Skatole.htmlhttps://www.MedChemExpress.com/StemRegenin-1.htmlhttps://www.MedChemExpress.com/Tapinarof.html


CCRCC chemokine receptor

CCR (Chemokine receptors) are cytokine receptors found on thesurface of certain cells that interact with a type of cytokine calledachemokine. There have been 19 distinct chemokine receptorsdescribed in mammals. Each has a 7-transmembrane (7TM) structureand couples to G-protein for signal transduction within a cell, makingthem members of a large protein family of G protein-coupledreceptors. Following interaction with their specific chemokine ligands,chemokine receptors trigger a flux in intracellular calcium (Ca ) ions2+

(calcium signaling). This causes cell responses, including the onset ofa process known as chemotaxis that traffics the cell to a desiredlocation within the organism. Chemokine receptors are divided into

different families, CXC chemokine receptors, CC chemokine receptors, CX3C chemokine receptors and XC chemokinereceptors that correspond to the 4 distinct subfamilies of chemokines they bind. Specific chemokine receptors providethe portals for HIV to get into cells, and others contribute to inflammatory diseases and cancer.

https://www.MedChemExpress.com/Targets/CCR.html

Purity: >98%Clinical Data: No Development ReportedSize: 250 mg, 500 mg



Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg


10 mg, 50 mg


10 mg, 50 mg


2 mg, 5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 20 mg



CCR Inhibitors & Modulators

Bioactivity: Aplaviroc, a SDP derivative, is a antagonist, with CCR5 IC s50of 0.1-0.4 nM for HIV-1 , HIV-1 and HIV-1 .Ba-L JRFL MOKW

Bioactivity: AZ084 is a potent, selective, allosteric and oral active CCR8antagonist, with a of 0.9 nM. Has potential to treat asthmaKi

.[1]

Bioactivity: AZD2098 is a potent and selective CC-chemokine receptor 4 inhibitor with s of 7.8, 8.0, 8.0 and 7.6 for(CCR4) pIC50

human, rat, mouse and dog respectively, used for asthmaresearch .[1] [2]

Bioactivity: BMS-813160 is the first dual antagonist to enterCCR2/CCR5clinical development for cardiovascular.

Bioactivity: BX471 (ZK-811752) is a potent and selective non-peptide CCR1antagonist with a of 1 nM, and exhibits 250-foldKiselectivity for CCR1 over CCR2, CCR5 and CXCR4.

Bioactivity: BX471 hydrochloride (ZK-811752 hydrochloride) is a potent,selective non-peptide antagonist with of 1 nM forCCR1 Kihuman CCR1, and exhibits 250-fold selectivity for CCR1 overCCR2, CCR5 and CXCR4.

Bioactivity: CCR1 antagonist 1 is an antagonist of , withCCR1anti-inflammatory activity.

Bioactivity: CCR1 antagonist 6 (compound 16q) is a chemokine receptor 1 antagonist, with an of 3 nM .(CCR1) IC50

[1]

Bioactivity: CCR1 antagonist 7 (compound 16r) is a chemokine receptor 1 antagonist, with an of 4 nM .(CCR1) IC50

[1]Bioactivity: CCR1 antagonist 8 (compound 19n), a third azaindazole series

compound, is a antagonist clinical candidate, with anCCR1 of 1.8 nM in Ca flux assay .IC50

2+ [1]


Aplaviroc (AK 602; GSK 873140; GW 873140) Cat. No.: HY-17450

AZ084 Cat. No.: HY-119217

AZD2098 Cat. No.: HY-U00064

BMS-813160 Cat. No.: HY-109593

BX471 (ZK-811752) Cat. No.: HY-12080

BX471 hydrochloride (ZK-811752 (hydrochloride)) Cat. No.: HY-12080A

CCR1 antagonist 1 Cat. No.: HY-U00350

CCR1 antagonist 6 Cat. No.: HY-114193



https://www.MedChemExpress.com/Targets/CCR.htmlhttps://www.MedChemExpress.com/Aplaviroc.htmlhttps://www.MedChemExpress.com/az084.htmlhttps://www.MedChemExpress.com/AZD2098.htmlhttps://www.MedChemExpress.com/BMS-813160.htmlhttps://www.MedChemExpress.com/BX471.htmlhttps://www.MedChemExpress.com/BX471-hydrochloride.htmlhttps://www.MedChemExpress.com/Ethanone,_1-[4-_4-chloro-3-methoxyphenyl_-1-piperazinyl]-2-[3-_1H-imidazol-2-yl_-1H-pyrazolo[3,4-b]pyridin-1-yl]-.htmlhttps://www.MedChemExpress.com/ccr1-antagonist-6.htmlhttps://www.MedChemExpress.com/ccr1-antagonist-7.htmlhttps://www.MedChemExpress.com/CCR1_antagonist_8.html



5 mg, 10 mg, 25 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg

Purity: 98.73%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 25 mg


1 mg, 5 mg, 10 mg, 25 mg, 50 mg


1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


Purity: >98%Clinical Data: No Development ReportedSize: 20 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


Bioactivity: CCR2 antagonist 1 is a high-affinity and long-residence-time antagonist, with a of 2.4 nM.CCR2 Ki

Bioactivity: CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine with an of 103 nM.receptor type 2 (CCR2) IC50

Bioactivity: CCR3 antagonist 1 is a potent antagonist of , used forCCR3the research of immunologic and inflammatory diseases.

Bioactivity: CCR5 antagonist 1 is a antagonist which can inhibit CCR5 HIVreplication extracted from WO 2004054974 A2.

Bioactivity: CCR6 inhibitor 1 is a potent and selective inhibitor,CCR6with s of 0.45 and 6 nM for monkey and human CCR6, muchIC50more selective at CCR6 over human CCR1 (IC , > 3000050nM), and CCR7 (IC , 9400 nM). CCR6 inhibitor 1 marke…50

Bioactivity: Cenicriviroc is an orally active, dual antagonist,CCR2/CCR5also inhibits both HIV-1 and HIV-2, and displays potentanti-inflammatory and antiinfective activity.

Bioactivity: Cenicriviroc is a dual antagonist, also inhibitsCCR2/CCR5both HIV-1 and HIV-2, and displays potent anti-inflammatoryand antiinfective activity.

Bioactivity: DAPTA is a synthetic peptide, functions as a viral entryinhibitor by targeting selectively , and shows potentCCR5anti-HIV activities.

Bioactivity: GSK2239633A is a CC-chemokine receptor 4 ( ) antagonist,CCR4which inhibits the binding of [ I]-TARC to human CCR4 with a125

of 7.96±0.11.pIC50

Bioactivity: GW 766994 is a specific and oral chemokine receptor-3 antagonist, which has entered clinical trial for(CCR3)

asthma and eosinophilic bronchitis.


CCR2-RA-[R] Cat. No.: HY-50081

CCR3 antagonist 1 Cat. No.: HY-U00331


CCR6 inhibitor 1 Cat. No.: HY-112701

Cenicriviroc (TAK-652; TBR-652) Cat. No.: HY-14882

Cenicriviroc Mesylate (TAK-652 Mesylate; TBR-652 Mesylate) Cat. No.: HY-14882A

DAPTA (D-Ala-peptide T-amide; Adaptavir) Cat. No.: HY-P1034

GSK2239633A Cat. No.: HY-100183

GW 766994 (GW 994) Cat. No.: HY-107051

https://www.MedChemExpress.com/CCR2_antagonist_1.htmlhttps://www.MedChemExpress.com/CCR2-RA--R-.htmlhttps://www.MedChemExpress.com/4-Thiazoleacetic_acid,_2-[[2-[[[_2S_-4-[_3,4-dichlorophenyl_methyl]-2-morpholinyl]methyl]amino]-2-oxoethyl]thio]-.htmlhttps://www.MedChemExpress.com/CCR5_antagonist_1.htmlhttps://www.MedChemExpress.com/CCR6_inhibitor_1.htmlhttps://www.MedChemExpress.com/Cenicriviroc.htmlhttps://www.MedChemExpress.com/Cenicriviroc_Mesylate.htmlhttps://www.MedChemExpress.com/DAPTA.htmlhttps://www.MedChemExpress.com/GSK2239633A.htmlhttps://www.MedChemExpress.com/GW_766994.html


10 mg, 50 mg



5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg

Purity: 99.75%Clinical Data: Phase 2Size: 5 mg, 10 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg



10 mg, 50 mg

Bioactivity: INCB 3284 is a potent, selective and orally bioavailable human antagonist, inhibiting monocyte chemoattractantCCR2

protein-1 binding to , with an of 3.7 nM. INCB 3284hCCR2 IC50can be used in the research of acute liver failure.

Bioactivity: INCB 3284 dimesylate is a potent, selective and orallybioavailable human antagonist, inhibiting monocyteCCR2chemoattractant protein-1 binding to , with an ofhCCR2 IC503.7 nM. INCB 3284 dimesylate can be used in the research ofacute liver failure.

Bioactivity: INCB3344 is a potent, selective and orally bioavailable CCR2antagonist with values of 5.1 nM (hCCR2) and 9.5 nMIC50(mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM(mCCR2) in antagonism of chemotaxis activity.

Bioactivity: Maraviroc is a selective antagonist with activityCCR5against human .HIV

Bioactivity: MK-0812 is a potent and selective antagonist with low nMCCR2affinity for CCR2.

Bioactivity: MK-0812 Succinate is a potent and selective antagonistCCR2with high affinity at CCR2.

Bioactivity: PF-4136309 is a potent, selective, and orally bioavailable antagonist, with s of 5.2 nM, 17 nM and 13 nM forCCR2 IC50

human, mouse and rat CCR2.

Bioactivity: RS 504393 is a selective chemokine receptor antagonist (CCR2 values are 89 nM and > 100 μM for inhibition of humanIC50

recombinant CCR2 and CCR1 receptors respectively).

Bioactivity: RS102895 is a potent antagonist, with an of 360 nM,CCR2 IC50and shows no effect on CCR1.

Bioactivity: RS102895 hydrochloride is a potent antagonist, with anCCR2 of 360 nM, and shows no effect on CCR1.IC50


INCB 3284 Cat. No.: HY-15450A

INCB 3284 dimesylate Cat. No.: HY-15450

INCB3344 Cat. No.: HY-50674

Maraviroc (UK-427857) Cat. No.: HY-13004

MK-0812 Cat. No.: HY-50669

MK-0812 Succinate Cat. No.: HY-50669A

PF-4136309 (INCB8761) Cat. No.: HY-13245

RS 504393 Cat. No.: HY-15418

RS102895 Cat. No.: HY-18611A

RS102895 hydrochloride Cat. No.: HY-18611

https://www.MedChemExpress.com/INCB-3284.htmlhttps://www.MedChemExpress.com/incb-3284-dimesylate.htmlhttps://www.MedChemExpress.com/INCB3344.htmlhttps://www.MedChemExpress.com/Maraviroc.htmlhttps://www.MedChemExpress.com/mk-0812.htmlhttps://www.MedChemExpress.com/MK-0812-Succinate.htmlhttps://www.MedChemExpress.com/PF-4136309.htmlhttps://www.MedChemExpress.com/rs-504393.htmlhttps://www.MedChemExpress.com/RS102895.htmlhttps://www.MedChemExpress.com/RS102895-hydrochloride.html



5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg


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5 mg


5 mg, 10 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Bioactivity: SB297006 is a antagonist, which significantly inhibitsCCR3proliferation and neurosphere formation in CCL11-treatedneural progenitor cells.

Bioactivity: TAK-220 is a selective and orally bioavailable CCR5antagonist, with s of 3.5 nM and 1.4 nM for inhibition onIC50the binding of RANTES and MIP-1α to CCR5, respectively, butshows no effect on the binding to CCR1, CCR2b, CCR3, CCR4,…

Bioactivity: TAK-779 is a potent and selective nonpeptide antagonist of and , with a of 1.1 nM for CCR5, andCCR5 CXCR3 Ki

effectively and selectively inhibits , with …R5 HIV-1 EC50

Bioactivity: Teijin compound 1 is a specific antagonist with sCCR 2 IC50of 24 and 180 nM in chemotaxis and binding assay,respectively.

Bioactivity: Vercirnon is an orally bioavailable, selective, and potentantagonist of , with an of 10 nM, used in theCCR9 IC50research of inflammatory bowel diseases.

Bioactivity: Vicriviroc maleate is a potent, selective, oral bioavailableand CNS penetrated antagonist of , with a of 2.5 nM,CCR5 Kiand also inhibits HIV-1 in PBMC cells, with s of 3.3 nMIC90(JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) …

Bioactivity: ZK756326 dihydrochloride is a nonpeptide chemokine receptoragonist for the CC chemokine receptor .CCR8

SB297006 Cat. No.: HY-103361

TAK-220 Cat. No.: HY-19974

TAK-779 (Takeda 779) Cat. No.: HY-13406

Teijin compound 1 Cat. No.: HY-108323

Vercirnon (GSK-1605786; CCX282-B; Traficet-EN) Cat. No.: HY-15724

Vicriviroc maleate (SCH-417690 (maleate); SCH-D (maleate)) Cat. No.: HY-17377

ZK756326 dihydrochloride Cat. No.: HY-101038A

https://www.MedChemExpress.com/SB297006.htmlhttps://www.MedChemExpress.com/TAK-220.htmlhttps://www.MedChemExpress.com/TAK-779.htmlhttps://www.MedChemExpress.com/Teijin_compound_1.htmlhttps://www.MedChemExpress.com/Vercirnon.htmlhttps://www.MedChemExpress.com/Vicriviroc-maleate.htmlhttps://www.MedChemExpress.com/ZK756326dihydrochloride.html

CD73ecto-5′-nucleotidase, NT5E

CD73 (Ecto-5′-nucleotidase), a component of the purinergic signalingpathway, is a 70-kD glycosylphosphatidylinositol-anchored cellsurface protein encoded by the NT5E gene.CD73 has both enzymatic and non-enzymatic functions in cells. As anucleotidase, CD73 catalyzes the hydrolysis of AMP into adenosineand phosphate, and CD73-generated adenosine plays an importantrole in tumor immunoescape. CD73 plays a crucial role in switchingon adenosinergic signaling. CD73 also functions as a signal andadhesive molecule that can regulate cell interaction with extracellularmatrix components, such as laminin and fibronectin, to mediate theinvasive and metastatic properties of cancers. Both the enzymatic and

non-enzymatic functions of CD73 are involved in cancer-associated processes and are not completely independent ofeach other.Overexpression of CD73 is associated with resistance to antitumor agents. Knockdown of CD73 inhibits in vitro cellgrowth, cell cycle progression and cell migration in many cancers. CD73 and its associated pathways may be useful astherapeutic targets.


https://www.MedChemExpress.com/Targets/cd73.html



5 mg, 10 mg, 25 mg

Purity: >98%Clinical Data: No Development ReportedSize:



1 mg, 5 mg, 10 mg, 25 mg, 50 mg


CD73 Inhibitors & Modulators

Bioactivity: AB-680 is highly potent, reversible and selective smallmolecule inhibitor of (an ecto-nucleotidase), with a CD73 Kiof 4.9 pM for hCD73, displays >10,000-fold selectivity overrelated ecto-nucleotidases CD39. Anti-tumor activity .[1]

Bioactivity: CD73-IN-1 is an inhibitor of which can be used in theCD73treatment of cancer extracted from patent WO 2017153952 A1,example 80.

Bioactivity: MethADP is a specific inhibitor.CD73 Bioactivity: MethADP (sodium salt) is a specific inhibitor.CD73

Bioactivity: PSB-12379 is a potent ( ) inhibitorEcto-5'-Nucleotidase CD73with s of 9.03 nM (rat) and 2.21 nM (human).Ki

AB-680 Cat. No.: HY-125286

CD73-IN-1 Cat. No.: HY-103695

MethADP (Adenosine 5'-(α,β-methylene)diphosphate) Cat. No.: HY-112502

MethADP sodium salt Cat. No.: HY-112502B

PSB-12379 Cat. No.: HY-100747

https://www.MedChemExpress.com/Targets/CD73.htmlhttps://www.MedChemExpress.com/AB-680.htmlhttps://www.MedChemExpress.com/CD73-IN-1.htmlhttps://www.MedChemExpress.com/MethADP.htmlhttps://www.MedChemExpress.com/methadp-sodium-salt.htmlhttps://www.MedChemExpress.com/PSB-12379.html

Complement System

The complement system helps or “complements” the ability ofantibodies and phagocytic cells to clear pathogens from an organism.It is part of the immune system called the innate immune system thatis not adaptable and does not change over the course of anindividual's lifetime. The complement system consists of a number ofsmall proteins found in the blood, in general synthesized by the liver,and normally circulating as inactive precursors (pro-proteins). Whenstimulated by one of several triggers, proteases in the system cleavespecific proteins to release cytokines and initiate an amplifyingcascade of further cleavages. The end-result of this activation cascadeis massive amplification of the response and activation of the

cell-killing membrane attack complex. Over 30 proteins and protein fragments make up the complement system.Three biochemical pathways activate the complement system: the classical complement pathway, the alternativecomplement pathway, and the lectin pathway.


https://www.MedChemExpress.com/Targets/Complement System.html



5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: 98.89%Clinical Data: No Development ReportedSize: 500u g, 1 mg, 5 mg

Purity: >98%Clinical Data: No Development ReportedSize: 500u g, 1 mg, 5 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


Purity: 98.36%Clinical Data: No Development ReportedSize: 500u g, 1 mg, 5 mg



5 mg, 10 mg



5 mg, 10 mg, 50 mg, 100 mg

Complement System Inhibitors & Modulators

Bioactivity: Avacopan (CCX168) is a potent, selective and orally available 5a receptor inhibitor with an of 0.1 nM.complement IC50

Bioactivity: BCX 1470 inhibits the esterolytic activity of factor D(IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better,respectively, than that of trypsin. IC50 Value: 96 nM (FactorD); 1.6 nM (C1s); 326 nM (Trypsin) [1] Target: Factor D; C1sBCX 1470(Thrombin inhibitor) is serine protease inhibitor.BCX…

Bioactivity: BCX 1470 methanesulfonate inhibits the esterolytic activity offactor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-foldbetter, respectively, than that of trypsin. IC50 Value: 96 nM(Factor D); 1.6 nM (C1s); 326 nM (Trypsin) [1] Target: FactorD; C1s BCX 1470 is serine protease inhibitor. BCX 1470 blocks…

Bioactivity: C3a (70-77) is an octapeptide corresponding to the COOHterminus of C3a, exhibits the specificity and 1 to 2% biologicactivities of C3a.

Bioactivity: Compstatinis is a 13-residue cyclic peptide, and a potentinhibitor of the .complement system

Bioactivity: FD-IN-1 (Compound 12) is a ( ) inhibitor with anfactor D FDof 12 nM. Complement FD, a highly specific S1 serineIC 50

protease, plays a central role in the alternative complementpathway of the innate immune system. FD-IN-1 also inhib…

Bioactivity: Leukadherin-1 is a specific agonist of and the leukocyteCR3surface integrin CD11b/CD18.

Bioactivity: PMX 205 is a potent ( ;complement C5a receptor C5aR) antagonist.CD88

Bioactivity: PMX 205 Trifluoroacetate is a potent complement C5a ( ; ) antagonist.receptor C5aR CD88

Bioactivity: SB290157 trifluoroacetate is a potent and selective C3areceptor antagonist with an of 200 nM.IC50

Avacopan (CCX168) Cat. No.: HY-17627

BCX 1470 Cat. No.: HY-50874

BCX 1470 methanesulfonate Cat. No.: HY-50875

C3a 70-77 (Complement 3a (70-77)) Cat. No.: HY-P1505

Compstatin Cat. No.: HY-P1036

FD-IN-1 Cat. No.: HY-128570

Leukadherin-1 Cat. No.: HY-15701

PMX 205 Cat. No.: HY-110136

PMX 205 Trifluoroacetate Cat. No.: HY-110136A

SB290157 trifluoroacetate Cat. No.: HY-101502A

https://www.MedChemExpress.com/Targets/Complement System.htmlhttps://www.MedChemExpress.com/Avacopan.htmlhttps://www.MedChemExpress.com/bcx-1470.htmlhttps://www.MedChemExpress.com/bcx-1470-methanesulfonate.htmlhttps://www.MedChemExpress.com/C3a_70-77.htmlhttps://www.MedChemExpress.com/Compstatin.htmlhttps://www.MedChemExpress.com/fd-in-1.htmlhttps://www.MedChemExpress.com/Leukadherin-1.htmlhttps://www.MedChemExpress.com/PMX_205.htmlhttps://www.MedChemExpress.com/PMX_205_Trifluoroacetate.htmlhttps://www.MedChemExpress.com/SB290157_trifluoroacetate.html


1 mg, 5 mg, 10 mg, 50 mg

Bioactivity: W-54011 is a potent, specific, and orally active CD88 (C5areceptor) antagonist. W-54011 inhibits the binding of125I-labeled C5a to human neutrophils with a Ki value of 2.2nM. IC50 value: 2.2 nM (Ki) Target: CD88 (C5a receptor) invitro: W-54011 also inhibits C5a-induced intracellular Ca2+…


W-54011 Cat. No.: HY-16992A

https://www.MedChemExpress.com/W-54011.html


COXCyclooxygenase

Cyclooxygenase (COX), officially known asprostaglandin-endoperoxide synthase (PTGS), is an enzyme that isresponsible for formation of important biological mediators calledprostanoids, including prostaglandins, prostacyclin and thromboxane.Pharmacological inhibition of COX can provide relief from thesymptoms of inflammation and pain. Drugs, like Aspirin, that inhibitcyclooxygenase activity have been available to the public for about100 years. Two cyclooxygenase isoforms have been identified and arereferred to as COX-1 and COX-2. Under many circumstances theCOX-1 enzyme is produced constitutively (i.e., gastric mucosa)whereas COX-2 is inducible (i.e., sites of inflammation). Non-steroidal

anti-inflammatory drugs (NSAID), such as aspirin and ibuprofen, exert their effects through inhibition of COX. Themain COX inhibitors are the non-steroidal anti-inflammatory drugs (NSAIDs).

https://www.MedChemExpress.com/Targets/COX.html


10 mg, 50 mg


100 mg

Purity: 99.69%Clinical Data: LaunchedSize: 5 g, 10 g


1 g, 5 g


1 g, 5 g

Purity: 99.99%Clinical Data: No Development ReportedSize: 1 g, 5 g


5 mg, 10 mg, 25 mg, 50 mg


10 mg, 50 mg, 100 mg


5 mg, 10 mg


100 mg

COX Inhibitors & Modulators

Bioactivity: (+)-Catechin hydrate inhibits cyclooxygenase-1 ( ) withCOX-1an of 1.4 μM.IC50

Bioactivity: (-)-Catechin gallate is a minor constituent in green teacatechins. (-)-Catechin gallate inhibits the activity of

and enzymes.COX-1 COX-2

Bioactivity: (-)-Epicatechin inhibits cyclooxygenase-1 ( ) with anCOX-1 of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-inducedIC50

expression of iNOS by blocking the nuclear localization of thep65 subunit of NF-κB.

Bioactivity: Epicatechin gallate inhibits cyclooxygenase-1 ( ) withCOX-1an of 7.5 μM.IC50

Bioactivity: (S)-(+)-Ibuprofen is the S-enantiomer of Ibuprofen. Ibuprofenis an anti-inflammatory inhibitor targeting and COX-1 COX-2with of 13 μM and 370 μM, respectively.IC50

Bioactivity: Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID)analog of Diclofenac. Target: COX Aceclofenac is anon-steroidal anti-inflammatory drug (NSAID) analog ofDiclofenac. It is used for the relief of pain and inflammationin rheumatoid arthritis, osteoarthritis and ankylosing…

Bioactivity: Acemetacin (TVX 1322) is a non-steroidal anti-inflammatorydrug and a glycolic acid ester of indometacin that is acyclooxygenase inhibitor.

Bioactivity: Acetaminophen (paracetamol) is a selective cyclooxygenase-2 () inhibitor with an of 25.8 μM; is a widely usedCOX-2 IC50

antipyretic and analgesic drug.

Bioactivity: Adelmidrol exerts important anti-inflammatory effects that arepartly dependent on . Adelmidrol reduces PPARγ NF-κBtranslocation, and expression.COX-2

Bioactivity: Amfenac Sodium Hydrate is a inhibitor.COX-2


(+)-Catechin hydrate Cat. No.: HY-N0355

(-)-Catechin gallate ((-)-Catechin 3-gallate; (-)-Catechin 3-O-gallate) Cat. No.: HY-N0356

(-)-Epicatechin ((-)-Epicatechol; Epicatechin; epi-Catechin) Cat. No.: HY-N0001

(-)-Epicatechin gallate (ECG; Epicatechin gallate; (-)-Epicatechin 3-O-gallate) Cat. No.: HY-N0002

(S)-(+)-Ibuprofen ((S)-Ibuprofen) Cat. No.: HY-78131A

Aceclofenac Cat. No.: HY-B0634

Acemetacin (TVX 1322) Cat. No.: HY-B0482

Acetaminophen (Paracetamol; 4'-Hydroxyacetanilide; 4-Acetamidophenol; APAP) Cat. No.: HY-66005

Adelmidrol Cat. No.: HY-B1026

Amfenac Sodium Hydrate Cat. No.: HY-17479A

https://www.MedChemExpress.com/Targets/COX.htmlhttps://www.MedChemExpress.com/__addition__-Catechin_hydrate.htmlhttps://www.MedChemExpress.com/_-_-Catechin-gallate.htmlhttps://www.MedChemExpress.com/_-_-Epicatechin.htmlhttps://www.MedChemExpress.com/_-_-Epicatechin-gallate.htmlhttps://www.MedChemExpress.com/_S_-__addition__-Ibuprofen.htmlhttps://www.MedChemExpress.com/Aceclofenac.htmlhttps://www.MedChemExpress.com/acemetacin.htmlhttps://www.MedChemExpress.com/acetaminophen.htmlhttps://www.MedChemExpress.com/Adelmidrol.htmlhttps://www.MedChemExpress.com/Amfenac_Sodium_Hydrate.html




5 mg, 10 mg, 25 mg, 50 mg


100 mg, 1 g


10 mg, 50 mg, 100 mg


100 mg


10 mg, 50 mg, 100 mg


1 g, 5 g

Purity: 99.68%Clinical Data: No Development ReportedSize: 100 mg


1 g


10 mg, 50 mg

Bioactivity: Ampiroxicam(CP65703) is a nonselective cyclooxygenaseinhibitor uesd as anti-inflammatory drug. Target: COXAmpiroxicam is a non-steroidal anti-inflammatory drug. It is aprodrug of piroxicam. Ampiroxicam inhibits the stretchingresponse in mice induced by phenylbenzoquinone (PBQ) with…

Bioactivity: Ampyrone is a reagent for glucose determination in thepresence of peroxidase and phenol.

Bioactivity: Asarylaldehyde is a natural inhibitor, which isolatedCOX-2from carrot ( L.) seeds significantly inhibitsDaucus carotacyclooxygenase II (COX-2) activity at value 100 μg/mL.IC50

Bioactivity: Aspirin is a non-selective and irreversible inhibitor of and with s of 5 and 210 μg/mL.COX-1 COX-2 IC50

Bioactivity: ATB-346 is a novel hydrogen sulphide-releasing derivative ofnaproxen with markedly reduced toxicity. IC50 value: Target:COX-2 ATB-346 suppressed gastric prostaglandin E(2) synthesisas effectively as naproxen, but produced negligible damage inthe stomach and intestine, Unlike naproxen and celecoxib,…

Bioactivity: Carprofen is a nonsteroid anti-inflammatory agent, acts as amulti-target inhibitor, with s of 3.9 μM, 22.3FAAH/COX IC50μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.

Bioactivity: Catechin inhibits cyclooxygenase-1 ( ) with an ofCOX-1 IC501.4 μM.

Bioactivity: Celecoxib is a selective inhibitor with an of 40COX-2 IC50nM.

Bioactivity: Columbin is a diterpenoid furanolactone with anti-inflammationactivity.

Bioactivity: COX-2-IN-1 is potent and slective inhibitor with anCOX-2 of 3.9 μM.IC50

Ampiroxicam (CP 65703) Cat. No.: HY-17484

Ampyrone (4-Aminoantipyrine) Cat. No.: HY-B1398

Asaraldehyde (Asaronaldehyde; Asaraldehyde; 2,4,5-trimethoxy-Benzaldehyde) Cat. No.: HY-100580

Aspirin (ASA; Acetylsalicylic Acid) Cat. No.: HY-14654

ATB-346 Cat. No.: HY-15028

Carprofen Cat. No.: HY-B1227

Catechin ((+)-Catechin; Cianidanol; Catechuic acid) Cat. No.: HY-N0898

Celecoxib (SC 58635) Cat. No.: HY-14398

Columbin Cat. No.: HY-N0389

COX-2-IN-1 Cat. No.: HY-U00275

https://www.MedChemExpress.com/Ampiroxicam.htmlhttps://www.MedChemExpress.com/4-Aminoantipyrine.htmlhttps://www.MedChemExpress.com/Asarylaldehyde.htmlhttps://www.MedChemExpress.com/aspirin.htmlhttps://www.MedChemExpress.com/ATB-346.htmlhttps://www.MedChemExpress.com/Carprofen.htmlhttps://www.MedChemExpress.com/Catechin.htmlhttps://www.MedChemExpress.com/Celecoxib.htmlhttps://www.MedChemExpress.com/Columbin.htmlhttps://www.MedChemExpress.com/1-_4-Sulfamylphenyl_-3-trifluoromethyl-5-_7-chloroindol-3-yl_-2-pyrazoline.html


1 mg, 5 mg


10 mg, 50 mg, 100 mg


50 mg, 100 mg


100 mg

Purity: 98.0%Clinical Data: LaunchedSize: 10mM x 1mL in Water,

5 g


5 g, 10 g


5 g, 10 g


100 mg, 500 mg



Bioactivity: COX-2-IN-2 is a selective and inducible inhibitor withCOX2an of 0.24 μM. COX-2-IN-1 is an anti-inflammatoryIC50compound with anti-inflammatory and analgesic activities.

Bioactivity: COX/5-LO-IN-1 is an inhibitor of andcylooxygenase, used for the research of inflammatory and5-lipoxygenase

allergic disease states.

Bioactivity: Deracoxib, a selective cyclooxygenase-2 inhibitor, is anon-narcotic, non-steroidal anti-inflammatory drug (NSAID).IC50 Value: 70 to 150 uM(inhibition of 3 osteosarcoma celllines) [1] Target: COX in vitro: Concentration of deracoxibrequired for 50% inhibition of cell viability (IC50) was…

Bioactivity: Diclofenac is a potent and nonselective anti-inflammatoryagent, acts as a inhibitor, with s of 4 nM, 1.3 nMCOX IC50for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM forovine COX-1 and COX-2, respectively.

Bioactivity: Diclofenac diethylamine is a potent and nonselectiveanti-inflammatory agent, acts as a inhibitor, with sCOX IC50of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and5.1, 0.84 μM for ovine COX-1 and COX-2, respectively.

Bioactivity: Diclofenac Sodium (GP 45840) is a potent and nonselectiveanti-inflammatory agent, acts as a inhibitor, with sCOX IC50of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and5.1, 0.84 μM for ovine COX-1 and COX-2, respectively.

Bioactivity: Diflunisal (MK-647) is a salicylate derivative withnonsteroidal anti-inflammatory and uricosuric properties,which is used alone as an analgesic and in rheumatoidarthritis patients. The mechanism of action of diflunisal isas a Cyclooxygenase ( ) Inhibitor.COX

Bioactivity: Etodolac (AY-24236) is a non-steroidal anti-inflammatorycompound that is a non-selective inhibitor of COX (IC =53.550nM)

Bioactivity: Etoricoxib (MK-0663) is a non steroidal anti-inflammatoryagent, acting as a selective and orally active COX-2inhibitor, with s of 1.1 μM and 116 μM for COX-2 and COX-1IC50in human whole blood.

Bioactivity: Etoricoxib D4 (MK-0663 D4) is a deuterium labeled Etoricoxib.Etoricoxib is a non steroidal anti-inflammatory agent, actingas a selective and orally active inhibitor, with sCOX-2 IC50of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blo…


COX-2-IN-2 Cat. No.: HY-101655

COX/5-LO-IN-1 Cat. No.: HY-U00347

Deracoxib (SC 046; SC 46; SC 59046) Cat. No.: HY-17509

Diclofenac Cat. No.: HY-15036

Diclofenac diethylamine Cat. No.: HY-15036A

Diclofenac Sodium (GP 45840) Cat. No.: HY-15037

Diflunisal (MK-647) Cat. No.: HY-18342

Etodolac (AY-24236) Cat. No.: HY-76251

Etoricoxib (MK-0663; L-791456) Cat. No.: HY-15321

Etoricoxib D4 (MK-0663 D4; L-791456 D4) Cat. No.: HY-15321S

https://www.MedChemExpress.com/1-_4-fluorophenyl_-5-[4-_methylsulfonyl_phenyl]-pyrazole-3-carbonitrile.htmlhttps://www.MedChemExpress.com/Urea,_N-[3-[5-[_4-fluorophenyl_methyl]-2-thienyl]-1-methyl-2-propyn-1-yl]-N-hydroxy-.htmlhttps://www.MedChemExpress.com/deracoxib.htmlhttps://www.MedChemExpress.com/Diclofenac.htmlhttps://www.MedChemExpress.com/diclofenac-diethylamine.htmlhttps://www.MedChemExpress.com/Diclofenac-Sodium.htmlhttps://www.MedChemExpress.com/Diflunisal.htmlhttps://www.MedChemExpress.com/etodolac.htmlhttps://www.MedChemExpress.com/Etoricoxib.htmlhttps://www.MedChemExpress.com/Etoricoxib-D4.html



100 mg, 500 mg



1 g, 5 g


100 mg



10 mg, 50 mg


5 mg, 10 mg, 50 mg


1 g, 5 g

Purity: >98%Clinical Data: LaunchedSize: 1 g, 5 g


1 g, 5 g

Bioactivity: Fenofibric acid, an active metabolite of fenofibrate, is a activitor, with s of 22.4 µM, 1.47 µM, and 1.06 µMPPAR EC50

for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid alsoinhibits enzyme activity, with an of 48 nM.COX-2 IC50

Bioactivity: Fenoprofen Calcium is a nonsteroidal, anti-inflammatoryantiarthritic agent. Target: Prostaglandin G/H synthase 1Fenoprofen is a non-steroidal anti-inflammatory, antipyretic,analgesic agent advocated for use in rheumatoid arthritis,degenerative joint disease, ankylosing spondylitis and gout.…

Bioactivity: Fenoprofen Calcium hydrate is a nonsteroidal,anti-inflammatory antiarthritic agent. Target: ProstaglandinG/H synthase 1 Fenoprofen is a non-steroidalanti-inflammatory, antipyretic, analgesic agent advocated foruse in rheumatoid arthritis, degenerative joint disease,…

Bioactivity: Firocoxib(ML 1785713) is a potent and selective cyclooxygenase(COX)-2 inhibitor with IC50 of 0.13 uM, 58 fold sensitivityfor COX2 VSCOX1. IC50 value: 0.13 uM [1] Target: COX2inhibitor in vitro: Blood concentrations resulting in 50%inhibition of COX-1 and COX-2 activity in vitro were 75 +/- 2…

Bioactivity: FK 3311 is a selective inhibitor of COX-2; antiinflammatoryagent. IC50 Value: 1.6 uM [1] Target: COX-2 Cyclooxygenase(COX) is an intracellular enzyme that converts arachidonicacid into prostaglandin (PG)G2 and PGH2. in vitro: The racemicmixtures and the (R)- and (S)-isomers of the 2 metabolites…

Bioactivity: Flosulide is a potent and selective inhibitor, used forCOX-2the treatment for inflammatory diseases.

Bioactivity: Flufenamic acid is a non-steroidal anti-inflammatory agent,inhibits cyclooxygenase ( ), activates , and alsoCOX AMPKmodulates ion channels, blocking and chloride channels L-type

, modulating non-selective cation channel…Ca channels2+

Bioactivity: Flunixin Meglumine is a potent inhibitor of COX used asanalgesic agent with anti-inflammatory and antipyreticactivity. Target: COX Flunixin meglumine is a potent,non-narcotic, non-steroidal analgesic agent withanti-inflammatory and antipyretic activity. It is a potent…

Bioactivity: FR-188582 is a highly selective inhibitor of (cyclooxygenase)-2, with an value of 17 nM.COX IC50

Bioactivity: Gallic acid is an antioxidant which can inhibit both .COX-2

Fenofibric acid (FNF acid) Cat. No.: HY-B0760

Fenoprofen Calcium Cat. No.: HY-B0288A

Fenoprofen Calcium hydrate (Fenoprofen calcium salt dihydrate) Cat. No.: HY-B0288B

Firocoxib (ML 1785713) Cat. No.: HY-14670

FK 3311 (COX-2 Inhibitor V) Cat. No.: HY-14445

Flosulide (ZK 38997; CGP 28238) Cat. No.: HY-U00083

Flufenamic acid Cat. No.: HY-B1221

Flunixin meglumine Cat. No.: HY-B0386

FR-188582 Cat. No.: HY-U00146

Gallic acid (3,4,5-Trihydroxybenzoic acid) Cat. No.: HY-N0523

https://www.MedChemExpress.com/Fenofibric-acid.htmlhttps://www.MedChemExpress.com/Fenoprofen-Calcium.htmlhttps://www.MedChemExpress.com/Fenoprofen-Calcium-hydrate.htmlhttps://www.MedChemExpress.com/Firocoxib.htmlhttps://www.MedChemExpress.com/FK-3311.htmlhttps://www.MedChemExpress.com/Flosulide.htmlhttps://www.MedChemExpress.com/Flufenamic-acid.htmlhttps://www.MedChemExpress.com/Flunixin-meglumine.htmlhttps://www.MedChemExpress.com/FR-188582.htmlhttps://www.MedChemExpress.com/Gallic_acid.html



5 mg, 10 mg, 50 mg


1 g, 5 g


5 mg


100 mg



10 mg, 50 mg, 100 mg


5 mg, 10 mg



5 mg, 10 mg

Bioactivity: Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibitsanti-inflammatory effects by reducing and .iNOS COX-2Ginsenoside C-K exhibits an inhibition against the activity of

and in human liver microsomes with s ofCYP2C9 CYP2A6 IC5032.0±3.6 μM and 63.6±4.2 μM, respectively.

Bioactivity: Ginsenoside Rb3 is extracted from steamed .Panax notoginsengGinsenoside Rb3 exhibits inhibitory effect on TNFα-induced

transcriptional activity with an of 8.2 μM in 293TNF-κB IC50cell lines. Ginsenoside Rb3 also inhibits the induction of

and mRNA.COX-2 iNOS

Bioactivity: Ginsenoside Rd inhibits TNFα-induced transcriptionalNF-κBactivity with an of 12.05±0.82 μM in HepG2 cells.IC50Ginsenoside Rd inhibits expression of and mRNA.COX-2 iNOSGinsenoside Rd also inhibits influx. Ginsenoside…Ca2+

Bioactivity: Ginsenoside Rg3 is the main component of Red ginseng.Ginsenoside Rg3 inhibits and channel with ICNa+ hKv1.4

s of 32.2±4.5 and 32.6±2.2 μM, respectively. Ginsenoside50Rg3 also inhibits levels, activity, and Aβ NF-κB COX-2




10 mg, 50 mg, 100 mg, 200 mg


100 mg, 200 mg, 500 mg


1 g, 5 g

Purity: >98%Clinical Data: LaunchedSize: 100 mg, 500 mg


1 g, 5 g


1 mg, 5 mg, 10 mg, 25 mg


1 mg, 5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg


1 g, 5 g

Bioactivity: Indomethacin is a potent and nonselective inhibitor of COX1and , with s of 18 nM and 26 nM for human COX-1 andCOX2 IC50COX-2, respectively, in CHO cells.

Bioactivity: Inulicin (1-O-Acetylbritannilactone) is an active compoundisolated from . InulicinInula Britannica L(1-O-Acetylbritannilactone) inhibits VEGF-mediated activationof and . Inulicin (1-O-Acetylbritannilactone)Src FAKinhibits LPS-induced production and expression,…PGE2 COX-2

Bioactivity: Isoorientin is a potent inhibitor of with an valueCOX-2 IC50of 39 μM.

Bioactivity: Jaceosidin is a flavonoid isolated from ,Artemisia vestitainduces apoptosis in cancer cells, activates andBaxdown-regulates Mcl-1 and c-FLIP expression . Jaceosidin[1]

exhibits anti-cancer , anti-inflammatory activiti…[2]

Bioactivity: Ketoprofen (RP-19583) is a non-steroidal antiinflammatoryagent, acting as a potent inhibitor of , with s of 2COX IC50nM and 26 nM for COX-1 and COX-2 in human blood monocytes,respectively.

Bioactivity: Ketorolac is a non-steroidal anti-inflammatory agent, actingas a nonselective inhibitor, with s of 20 nM forCOX IC50COX-1 and 120 nM for COX-2.

Bioactivity: Ketorolac tromethamine salt is a non-steroidalanti-inflammatory agent, acting as a nonselective COXinhibitor, with s of 20 nM for COX-1 and 120 nM for COX-2.IC50

Bioactivity: Lornoxicam, a COX-1 and COX-2 inhibitor, is a new nonsteroidalanti-inflammatory drug (NSAID). Target: COX Lornoxicam showeda balanced inhibition of COX-1/-2 exhibiting the lowest IC50(0.005 microM/0.008 microM) of the large panel of NSAIDstested. lornoxicam showed a marked inhibition of IL-6…

Bioactivity: Loxoprofen is a non-steroidal anti-inflammatory drug. Target:COX Loxoprofen is a non-steroidal anti-inflammatory drug inthe propionic acid derivatives group, which also includesibuprofen and naproxen among others. Loxoprofen is anon-selective cyclooxygenase inhibitor, and works by reducing…

Bioactivity: LY 178002 is a potent inhibitor of , 5-lipoxygenase phospholipase, with of 0.6 μM for 5-1ipoxygenase, inhibits cellularA2 IC50

production of LTB4 by human polymorphonuclear leukocytes, andshows relatively weak inhibition on .cyclooxygenase

Indomethacin (Indometacin) Cat. No.: HY-14397

Inulicin (1-O-Acetylbritannilactone) Cat. No.: HY-N0896

Isoorientin (Homoorientin) Cat. No.: HY-N0767

Jaceosidin Cat. No.: HY-N0831

Ketoprofen (RP-19583) Cat. No.: HY-B0227

Ketorolac (RS37619) Cat. No.: HY-B0580

Ketorolac tromethamine salt (Ketorolac tris salt; Ketorolac Tromethamine; RS37619 tromethamine salt) Cat. No.: HY-B0138

Lornoxicam (Chlortenoxicam; Ro 13-9297; TS110) Cat. No.: HY-B0367

Loxoprofen Cat. No.: HY-B0578

LY 178002 Cat. No.: HY-101579

https://www.MedChemExpress.com/Indomethacin.htmlhttps://www.MedChemExpress.com/1-O-Acetylbritannilactone.htmlhttps://www.MedChemExpress.com/Isoorientin.htmlhttps://www.MedChemExpress.com/Jaceosidin.htmlhttps://www.MedChemExpress.com/Ketoprofen.htmlhttps://www.MedChemExpress.com/ketorolac.htmlhttps://www.MedChemExpress.com/Ketorolac-tromethamine-salt.htmlhttps://www.MedChemExpress.com/Lornoxicam.htmlhttps://www.MedChemExpress.com/Loxoprofen.htmlhttps://www.MedChemExpress.com/LY_178002.html


10 mg, 50 mg, 100 mg


5 mg, 10 mg


5 g, 10 g

Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 g, 10 g


1 g, 5 g


50 mg

Purity: 98.0%Clinical Data: LaunchedSize: 500 mg


100 mg, 500 mg


5 g, 10 g

Bioactivity: Mefenamic acid is a non-steroidal anti-inflammatory agent,acting as a competitive inhibitor of and , withhCOX-1 hCOX-2

s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.IC50

Bioactivity: Meloxicam is a non-steroidal antiinflammatory agent, inhibits activity, with s of 0.49 µM and 36.6 µM for COX-2 andCOX IC50

COX-1, respectively.

Bioactivity: Metamizole (Dipyrone) sodium hydrate is a potent analgesicdrug that has been demonstrated to inhibit cyclooxygenase(COX).

Bioactivity: Methyl Salicylate (Wintergreen oil) is a topical analgesic andanti-inflammatory agent. Also used as a pesticide, adenaturant, a fragrance ingredient, and a flavoring agent infood and tobacco products . A systemic acquired resista…[1]

Bioactivity: Nabumetone is an orally active non-acidic anti-inflammatoryagent, acts as a potent and selective inhibitor, and isCOX-2the prodrug of the active metabolite 6MNA.

Bioactivity: Naproxen is a and inhibitor with s of 8.72COX-1 COX-2 IC50and 5.15 μM, respectively in cell assay.

Bioactivity: Naproxen etemesil is a lipophilic, non-acidic, inactiveprodrug of naproxen that is hydrolysed to pharmacologicallyactive Naproxen once absorbed. Naproxen is a and COX-1 COX-2inhibitor with s of 8.72 and 5.15 μM, respectively in cellIC50assay.

Bioactivity: Naproxen sodium is a and inhibitor with s ofCOX-1 COX-2 IC508.72 and 5.15 μM, respectively in cell assay.

Bioactivity: Neochlorogenic acid is a natural polyphenolic compound foundin dried fruits and other plants. Neochlorogenic acid inhibitsthe production of and . Neochlorogenic acidTNF-α IL-1βsuppresses protein expression. NeochlorogeniciNOS and COX-2acid also inhibits phosphorylated and …NF-κB p65 p38 MAPK

Bioactivity: Nepafenac(AHR 9434; AL 6515; Nevanac) is a selective COX-2inhibitor; is prodrug of Amfenac. IC50 value: Target: COX-2Nepafenac is a NSAID (nonsteroidal anti inflammatory drug)that is routinely used in opthamology to control painfollowing cataract surgery.


Mefenamic acid Cat. No.: HY-B0574

Meloxicam Cat. No.: HY-B0261

Metamizole sodium hydrate Cat. No.: HY-B1279

Methyl Salicylate (Wintergreen oil) Cat. No.: HY-Y0189

Nabumetone (BRL14777) Cat. No.: HY-B0559

Naproxen ((S)-Naproxen) Cat. No.: HY-15030

Naproxen etemesil (LT-NS 001; MX 1094) Cat. No.: HY-19675

Naproxen sodium Cat. No.: HY-15030A

Neochlorogenic acid (trans-5-O-Caffeoylquinic acid) Cat. No.: HY-N0722

Nepafenac (AHR 9434; AL 6515) Cat. No.: HY-17357

https://www.MedChemExpress.com/mefenamic-acid.htmlhttps://www.MedChemExpress.com/meloxicam.htmlhttps://www.MedChemExpress.com/Metamizole-sodium-hydrate.htmlhttps://www.MedChemExpress.com/Methyl_Salicylate.htmlhttps://www.MedChemExpress.com/Nabumetone.htmlhttps://www.MedChemExpress.com/Naproxen.htmlhttps://www.MedChemExpress.com/Naproxen_etemesil.htmlhttps://www.MedChemExpress.com/Naproxen-sodium.htmlhttps://www.MedChemExpress.com/Neochlorogenic-acid.htmlhttps://www.MedChemExpress.com/Nepafenac.html



25 mg, 50 mg, 100 mg


25 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg




10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 20 mg


100 mg, 500 mg


5 mg, 10 mg

Bioactivity: Nepafenac D5 is the deuterium labeled Nepafenac, which is aselective COX-2 inhibitor.

Bioactivity: Nimesulide is a selective inhibitor, with s of 70COX-2 IC50nM-70 μM in a time-dependent manner, but it shows no effect onCOX-1 (IC >100 μM). Nimesulide has potent50anti-inflammatory, analgesic and antipyretic properties.

Bioactivity: Nitroflurbiprofen is a ( ) inhibitor withcyclooxygenase COXnitric oxide (NO)-donating properties, modulates the increasedintrahepatic vascular tone in portal hypertensive cirrhoticrats.

Bioactivity: NS-398 is a non-steroidal an-inflammatory agent with analgesicand antipyretic effects, and selectively inhibitsprostaglandin G/H synthase 2/cyclooxygenase 2 ( )COX-2activity, with an of 3.8 μM, and has no effect on COX-1IC50at 100 μM.

Bioactivity: Oxaprozin is an inhibitor of both and with sCOX-1 COX-2 IC50of 2.2 μM and 36 μM for human platelet COX-1 andIL-1-stimulated human synovial cell COX-2, respectively.Oxaprozin also inhibits the activation of .NF-κB

Bioactivity: Oxaprozin D4 is the deuterium labeled Oxaprozin, which is anon-steroidal anti-inflammatory drug (NSAID).

Bioactivity: Pamicogrel (KBT3022) is a ( ) inhibitor.cyclooxygenase COX Bioactivity: Paradol is a pungent phenolic substance found in ginger andother Zingiberaceae plants. Paradol is an effective inhibitorof tumor promotion in mouse skin carcinogenesis, binds to

active site.cyclooxygenase (COX)-2

Bioactivity: Parecoxib is a potent and selective COX-2 inhibitor. IC50value: Target: COX-2 in vitro: The prodrug Parecoxib as wellas its active metabolite val have a specific affinity to thecannabinoid (CB) receptor measured in CB1-expressing HEK 293cells and rat brain tissue [1]. in vivo: Adult male…

Bioactivity: Parecoxib is a potent and selective COX-2 inhibitor. IC50value: Target: COX-2 in vitro: The prodrug Parecoxib as wellas its active metabolite val have a specific affinity to thecannabinoid (CB) receptor measured in CB1-expressing HEK 293cells and rat brain tissue [1]. in vivo: Adult male…

Nepafenac D5 (AHR-9434 D5; AL-6515 D5) Cat. No.: HY-17357S

Nimesulide (R805) Cat. No.: HY-B0363

Nitroflurbiprofen (HCT 1206; NO-flurbiprofen; Nitroxybutyl flurbiprofen) Cat. No.: HY-U00013

NS-398 Cat. No.: HY-13913

Oxaprozin (Oxaprozinum; Wy21743) Cat. No.: HY-B0808

Oxaprozin D4 (Wy-21743 D4) Cat. No.: HY-B0808S

Pamicogrel (KBT3022) Cat. No.: HY-U00175

Paradol ([6]-Gingerone; [6]-Paradol) Cat. No.: HY-14617

Parecoxib (SC 69124) Cat. No.: HY-17474

Parecoxib Sodium (SC 69124A) Cat. No.: HY-17474A

https://www.MedChemExpress.com/Nepafenac-D5.htmlhttps://www.MedChemExpress.com/nimesulide.htmlhttps://www.MedChemExpress.com/Nitroflurbiprofen.htmlhttps://www.MedChemExpress.com/NS-398.htmlhttps://www.MedChemExpress.com/Oxaprozin.htmlhttps://www.MedChemExpress.com/Oxaprozin-D4.htmlhttps://www.MedChemExpress.com/KB3022.htmlhttps://www.MedChemExpress.com/Paradol.htmlhttps://www.MedChemExpress.com/parecoxib.htmlhttps://www.MedChemExpress.com/Parecoxib-Sodium.html

Purity: 99.04%Clinical Data: No Development ReportedSize: 2 mg, 5 mg, 10 mg, 25 mg, 50 mg


100 mg



10 mg, 50 mg, 100 mg


100 mg


250 mg



1 g, 5 g, 10 g


500 mg


1 g, 5 g

Bioactivity: Phenacetin is a non-opioid analgesic without anti-inflammatoryproperties, inhibits COX-3 activity. Target: COX Phenacetin isa pain-relieving and fever-reducing drug, Phenacetin waswithdrawn from the Canadian market in June 1973 due toconcerns regarding nephropathy. the clinical and laboratory…

Bioactivity: Phenylbutazone is used as a non-steroidal anti-inflammatoryagent for the treatment of chronic pain, including thesymptoms of arthritis. Target: Others Phenylbutazone wasoriginally made available for use in humans for the treatmentof rheumatoid arthritis and gout in 1949. However, when…

Bioactivity: Piroxicam (CP-16171) is a non-steroidal anti-inflammatorydrugs, acts as a inhibitor, with s of 47, 25 μM forCOX IC50human monocyte COX-1 and COX-2, respectively.

Bioactivity: Prim-O-glucosylcimifugin exerts anti-inflammatory effectsthrough the inhibition of and expression by throughiNOS COX-2regulating JAK2/STAT3 signaling.

Bioactivity: Propyphenazone is a pyrazolone derivative withanti-inflammatory, analgesic and antipyretic activity,Propyphenazone-based analogues as prodrugs and selectivecyclooxygenase-2 inhibitors. TargetCOX-2 Propyphenazone isstructurally related to aminophenazone it has been associated…

Bioactivity: Rofecoxib is a potent, specific and orally active COX-2inhibitor, with s of 26 and 18 nM for human COX-2 in humanIC50osteosarcoma cells and Chinese hamster ovary cells, with a1000-fold selectivity for COX-2 over human COX-1 (IC &…50

Bioactivity: Rutaecarpine, an alkaloid of , is an inhibitorEvodia rutaecarpaof with an value of 0.28 μM.COX-2 IC50

Bioactivity: RWJ 63556 is an orally active COX-2 selective/5-lipoxygenaseinhibitor, with anti-inflammatory activities.

Bioactivity: S-(+)-Ketoprofen is a potent inhibitor of both andCOX-1 with s of 1.9 and 27 nM, respectively.COX-2 IC50

Bioactivity: S-(+)-Marmesin is a natural coumarin, exhibiting COX-2/5-LOXdual inhibitory activity.


Phenacetin (Acetophenetidin) Cat. No.: HY-B0476

Phenylbutazone Cat. No.: HY-B0230

Piroxicam (CP-16171) Cat. No.: HY-B0253

Prim-O-glucosylcimifugin Cat. No.: HY-N0635

Propyphenazone (4-Isopropylantipyrine; Isopropylphenazone) Cat. No.: HY-A0273

Rofecoxib (MK 966) Cat. No.: HY-17372

Rutaecarpine (Rutecarpine) Cat. No.: HY-N0147

RWJ 63556 Cat. No.: HY-U00022

S-(+)-Ketoprofen ((S)-Ketoprofen; Dexketoprofen) Cat. No.: HY-B2137

S-(+)-Marmesin ((+)-Marmesin; (S)-Marmesin) Cat. No.: HY-N2176

https://www.MedChemExpress.com/phenacetin.htmlhttps://www.MedChemExpress.com/phenylbutazone.htmlhttps://www.MedChemExpress.com/piroxicam.htmlhttps://www.MedChemExpress.com/Prim-O-glucosylcimifugin.htmlhttps://www.MedChemExpress.com/Propyphenazone.htmlhttps://www.MedChemExpress.com/Rofecoxib.htmlhttps://www.MedChemExpress.com/Rutaecarpine.htmlhttps://www.MedChemExpress.com/RWJ_63556.htmlhttps://www.MedChemExpress.com/S-__addition__-Ketoprofen.htmlhttps://www.MedChemExpress.com/S-__addition__-Marmesin.html




100 mg


100 mg, 500 mg


10 g, 50 g




5 mg, 10 mg, 25 mg, 50 mg, 100 mg


10 g, 50 g


500 mg, 1 g, 5 g


Bioactivity: S-2474 is an inhibitor of and , with sCOX-2 5-lipoxygenase IC50of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells,and used as a nonsteroidal anti-inflammatory drug.

Bioactivity: Salicin is a natural inhibitor.COX

Bioactivity: Salicylic acid inhibits cyclo-oxygenase-2 ( ) activityCOX-2independently of transcription factor (NF-κB) activation.

Bioactivity: SC-560 is a potent and selective inhibitor with an COX-1 IC50of 9 nM.

Bioactivity: SC57666 is a selective inhibitor with an of 26 nM.COX2 IC50 Bioactivity: SC58451 is a potent and selective inhibitor.Cox-2

Bioactivity: Sodium Salicylate inhibits cyclo-oxygenase-2 ( )COX-2activity independently of transcription factor (NF-κB)activation.

Bioactivity: Sulindac (MK-231) is a non-steroidal antiinflammatory agent,acts as a inhibitor, and inhibits overexpression ofCOX-2COX-2.

Bioactivity: Syringaldehyde is a polyphenolic compound belonging to thegroup of flavonoids and is found in different plant specieslike and .Manihot esculenta Magnolia officinalis [1]

Syringaldehyde moderately inhibits activity with…COX-2

Bioactivity: Tenidap, a non-steroidal anti-inflammatory drug, is aselective inhibitor, with values of 0.03 µM andCOX-1 IC501.2 µM for COX-1 and COX-2, respectively. Tenidap hasanti-inflammatory and antirheumatic properties .[1] [2]

S-2474 Cat. No.: HY-19212

Salicin (D-(−)-Salicin; Salicoside) Cat. No.: HY-N0149

Salicylic acid (2-Hydroxybenzoic acid) Cat. No.: HY-B0167

SC-560 Cat. No.: HY-59105

SC57666 Cat. No.: HY-U00129

SC58451 Cat. No.: HY-U00239

Sodium Salicylate (Salicylic acid sodium salt; 2-Hydroxybenzoic acid sodium salt) Cat. No.: HY-B0167A

Sulindac (MK-231) Cat. No.: HY-B0008

Syringaldehyde Cat. No.: HY-N1390

Tenidap (CP-66248) Cat. No.: HY-105028

https://www.MedChemExpress.com/S-2474.htmlhttps://www.MedChemExpress.com/Salicin.htmlhttps://www.MedChemExpress.com/Salicylic-acid.htmlhttps://www.MedChemExpress.com/SC-560.htmlhttps://www.MedChemExpress.com/SC57666.htmlhttps://www.MedChemExpress.com/SC58451.htmlhttps://www.MedChemExpress.com/Sodium-Salicylate.htmlhttps://www.MedChemExpress.com/Sulindac.htmlhttps://www.MedChemExpress.com/Syringaldehyde.htmlhttps://www.MedChemExpress.com/tenidap.html


100 mg


10 mg, 50 mg


5 mg, 10 mg, 50 mg


100 mg


1 g, 10 g





5 mg, 10 mg, 50 mg, 100 mg


1 g, 5 g

Bioactivity: Tenoxicam (Ro-12-0068), an antiinflammatory agent withanalgesic and antipyretic properties.

Bioactivity: TFAP is a selective cyclooxygenase-1 inhibitor, with(COX-1)an of 0.8 μM.IC50

Bioactivity: Thioflosulide (L-745337) is a selective cyclooxygenase-2 inhibitor, with an of 2.3 nM, and shows(COX2) IC50

anti-inflammatory activity.

Bioactivity: Tilmacoxib (JTE522) is a highly selective, time-dependent andirreversible human inhibitor with an of 85 nM inCOX-2 IC50an enzyme assay.

Bioactivity: Timegadine, a new antiinflammatory agent, is found to be apotent, competitive inhibitor of ( ) andcyclo-oxygenase COX

, with s ranging from 5 nM (washed rabbitlipo-oxygenase IC50platelets) to 20 μM (rat brain) for COX and 100 μM forlipo-oxygenase both in the cytosol fraction of horse platelet…

Bioactivity: Tolfenamic Acid (GEA 6414) is a non-steroidalanti-inflammatory and anti-cancer agent, selectively inhibits

, with an of 13.49 μM (3.53 μg/mL) in LPS-treatedCOX-2 IC50(COX-2) canine DH82 monocyte/macrophage cells, but shows noeffect on COX-1.

Bioactivity: Tolmetin sodium dihydrate is a non-steroidal antiinflammatoryagent, and acts as a non-selective inhibitor.COX

Bioactivity: Triflusal irreversibly inhibits the production ofthromboxane-B2 in platelets by acetylating cycloxygenase-1.Target: COX Triflusal at 10 mM, 100 mM and 1 M decreases LDHefflux in rat brain slices after anoxia/reoxygenation by 24%,35% and 49% respectively. Triflusal also reduces inducible NO…

Bioactivity: Valdecoxib is a highly potent and selective inhibitor of, with s of 5 nM and 140 μM for COX-2 and COX-1,COX-2 IC50

respeceively. Valdecoxib can be used in the research ofarthritis and pain.

Bioactivity: Veratric acid (3,4-Dimethoxybenzoic acid) is an orally activephenolic compound derived from vegetables and fruits, hasantioxidant and anti-inflammatory activities .[1] [3]

Veratric acid also acts as a protective agent agai…


Tenoxicam (Ro-12-0068) Cat. No.: HY-B0440

TFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) Cat. No.: HY-112731

Thioflosulide (L-745337) Cat. No.: HY-19217

Tilmacoxib (JTE522; JTP19605; RWJ57504) Cat. No.: HY-U00197

Timegadine (SR1368) Cat. No.: HY-100125

Tolfenamic Acid (GEA 6414) Cat. No.: HY-B0335

Tolmetin sodium dihydrate Cat. No.: HY-B1489

Triflusal Cat. No.: HY-B0531

Valdecoxib (SC 65872) Cat. No.: HY-15762

Veratric acid (3,4-Dimethoxybenzoic acid) Cat. No.: HY-N2007

https://www.MedChemExpress.com/tenoxicam.htmlhttps://www.MedChemExpress.com/TFAP.htmlhttps://www.MedChemExpress.com/L-745337.htmlhttps://www.MedChemExpress.com/JTE522.htmlhttps://www.MedChemExpress.com/Timegadine.htmlhttps://www.MedChemExpress.com/tolfenamic-acid.htmlhttps://www.MedChemExpress.com/Tolmetin-sodium-dihydrate.htmlhttps://www.MedChemExpress.com/triflusal.htmlhttps://www.MedChemExpress.com/Valdecoxib.htmlhttps://www.MedChemExpress.com/Veratric_acid.html



10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg

Bioactivity: Xanthohumol is one of the principal flavonoids isolated fromhops, the inhibitor of diacylglycerol acetyltransferase (

), and COX-2, and shows anti-cancer andDGAT COX-1anti-angiogenic activities.

Bioactivity: Zaltoprofen(CN100) is an inhibitor of COX for treatment ofarthritis. Target: COX Zaltoprofen, a preferential COX-2inhibitor, exhibited a potent inhibitory action on thenociceptive responses induced by a retrograde infusion ofbradykinin into the right common carotid artery in rats.…

Xanthohumol Cat. No.: HY-N1067

Zaltoprofen (CN100) Cat. No.: HY-B0619

https://www.MedChemExpress.com/Xanthohumol.htmlhttps://www.MedChemExpress.com/zaltoprofen.html

CXCRCXC chemokine receptors;C-X-C motif chemokine receptors

CXCRs (CXC chemokine receptors) are integral membrane proteinsthat specifically bind and respond to cytokines of the CXC chemokinefamily. They represent one subfamily of chemokine receptors, a largefamily of G protein-linked receptors that are known as seventransmembrane (7-TM) proteins, since they span thecell membraneseven times. There are currently seven known CXC chemokinereceptors in mammals, named CXCR1 through CXCR7. CXCR1 andCXCR2 are closely related receptors that recognize CXC chemokinesthat possess an E-L-R amino acid motif immediately adjacent to theirCXC motif. CXCR3 is expressed predominantly on T lymphocytes.CXCR4 is the receptor for a chemokine known as CXCL12 (or SDF-1)

and, as with CCR5, is utilized by HIV-1 to gain entry into target cells. The chemokine receptor CXCR5 is selectivelyexpressed on B cells and is involved in lymphocyte homing and the development of normal lymphoid tissue. CXCR6was formerly called three different names (STRL33, BONZO, and TYMSTR) before being assigned CXCR6 based on itschromosomal location and its similarity to other chemokine receptors in its gene sequence. CXCR7 was originallycalled RDC-1 (an orphan receptor) but has since been shown to cause chemotaxis in T lymphocytes in response toCXCL12 (the ligand for CXCR4) prompting the renaming of this molecule as CXCR7.


https://www.MedChemExpress.com/Targets/CXCR.html


Purity: >98%Clinical Data: No Development ReportedSize: 10mM x 1mL in Water,

5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg


10 mg, 50 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg




CXCR Inhibitors & Modulators

Bioactivity: ALX 40-4C is a small peptide inhibitor of the chemokine, inhibits SDF-1 from binding CXCR4 with a receptor CXCR4 Ki

of 1 μM, and suppresses the replication of X4 strains ofHIV-1; ALX 40-4C Trifluoroacetate also acts as an antagon…

Bioactivity: ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the, inhibits SDF-1 from bindingchemokine receptor CXCR4

CXCR4 with a of 1 μM, and suppresses the replication of X4Kistrains of HIV-1; ALX 40-4C Trifluoroacetate also acts as…

Bioactivity: AMD 3465 is a potent antagonist of , inhibits binding ofCXCR412G5 mAb and CXCL12 to , with s of 0.75 nMAF647 CXCR4 IC50and 18 nM in SupT1 cells; AMD 3465 also potently inhibits thereplication of strains ( : 1-10 nM), but has…X4 HIV IC50

Bioactivity: AMD 3465 hexahydrobromide is a potent antagonist of ,CXCR4inhibits binding of 12G5 mAb and CXCL12 to , withAF647 CXCR4

s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 alsoIC50potently inhibits the replication of strains ( X4 HIV IC50

Bioactivity: AMG 487 is an orally active and selective antagonist of CXCchemokine receptor 3 which inhibits the binding of(CXCR3)CXCL10 and CXCL11 to CXCR3 with s of 8.0 and 8.2 nM,IC50respectively.

Bioactivity: ATI-2341 is a agonist, induces CXCR4-dependent calciumCXCR4flux, with an of 194 nM in CCRF-CEM cells. ATI-2341 isEC50also a potent and efficacious mobilizer of bone marrowhematopoietic cells .[1]

Bioactivity: AZD-5069 is a potent antagonist,CXCR2 chemokine receptorused for caner treatment.

Bioactivity: AZD8797 is an allosteric non-competitive modulator of thehuman receptor; antagonizes CX3CR1 and CXCR2 with sCX3CR1 Kiof 3.9 and 2800 nM, respectively.

Bioactivity: Baohuoside I, a flavonoid isolated from Epimedium koreanum, acts as an inhibitor of , downregulates CXCR4Nakai CXCR4

expression, induces apoptosis and shows anti-tumor activity.

Bioactivity: Burixafor hydrobromide (TG-0054 hydrobromide) is an orallybioavailable and potent antagonist of and a well waterCXCR4soluble anti-angiogenic drug that is of potential value intreating choroid neovascularization . Burixafor[1]

hydrobromide (TG-0054 hydrobromide) mobilizes mesenchymalstem…

ALX 40-4C Cat. No.: HY-P7061

ALX 40-4C Trifluoroacetate Cat. No.: HY-P7061A

AMD 3465 (GENZ-644494) Cat. No.: HY-15971A

AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) Cat. No.: HY-15971

AMG 487 Cat. No.: HY-15319

ATI-2341 Cat. No.: HY-P0172

AZD-5069 Cat. No.: HY-19855

AZD8797 Cat. No.: HY-13848

Baohuoside I (Icariin-II; Icariside-II) Cat. No.: HY-N0011

Burixafor hydrobromide (TG-0054 hydrobromide) Cat. No.: HY-19867A

https://www.MedChemExpress.com/Targets/CXCR.htmlhttps://www.MedChemExpress.com/ALX_40-4C.htmlhttps://www.MedChemExpress.com/ALX_40-4C_Trifluoroacetate.htmlhttps://www.MedChemExpress.com/amd-3465.htmlhttps://www.MedChemExpress.com/AMD-3465-hexahydrobromide.htmlhttps://www.MedChemExpress.com/AMG-487.htmlhttps://www.MedChemExpress.com/ati-2341.htmlhttps://www.MedChemExpress.com/AZD-5069.htmlhttps://www.MedChemExpress.com/AZD8797.htmlhttps://www.MedChemExpress.com/Baohuoside-I.htmlhttps://www.MedChemExpress.com/Burixafor_hydrobromide.html

Purity: >98%Clinical Data: Phase 1Size: 2 mg, 5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 5 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg



1 mg, 5 mg, 10 mg, 50 mg, 100 mg


Purity: 98.81%Clinical Data: No Development ReportedSize: 10mM x 1mL

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Immunology/Inflammation - MedchemExpress.com · Immunology/Inflammation ... Besides resolving infection and injury, chronic inflammation is a risk factor for cancer. Immunity has