Ion Channels - Tocris Bioscience · 2017-06-19 · Ion channels are pore-forming proteins present in the plasma membrane of most cells, as well as the intracellular membranes surrounding

Ion Channels

Products by Gating Mechanism:• Ligand-gated Ion Channels• Voltage-gated Ion Channels• Other Ion Channels

Western Honey BeeApis melliferaA source of Apamin

Product Listing | Edition 1

Tocris Product Listing Series

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IntroductionIon channels are pore-forming proteins present in the plasma membrane of most cells, as well as the intracellular membranes surrounding many organelles, allowing the passage of ions across the membrane. They are essential for maintaining resting membrane potential, generating action potentials and other electrical signaling, and regulating cell volume. Ion channels have a fundamental role in physiological processes such as T cell activation, muscle contraction, insulin release from pancreatic β cells and transport of nutrients and ions across epithelial cells. A huge variety of ion channels exist, exhibiting selective permeability to particular ions and having different gating mechanisms. Ion channels may be classified according to their ion selectivity or gating mechanism, i.e. how the flow of ions is controlled. We have followed the IUPHAR classification of ion channels for the purposes of this listing and grouped the products into three main sections according to gating mechanism: Ligand-gated Ion Channels, Voltage-gated Ion Channels, and Other Channels.

Contents

Front cover image by Mikhail Laptev (https://www.dreamstime.com/royalty-free-stock-photography-honey-bee-apis-mellifera-dahlia-flower-image27164717) via dreamstime.com

Ligand-gated Ion Channels 3

5-HT3 4

AcetylcholineNicotinicReceptors 4

Nicotinic (α7) Receptors 4

Nicotinic (α4β2) Receptors 6

Nicotinic Receptors (Non-selective/Other) 7

Acid-sensingIonChannels 8

EpithelialSodiumChannels 8

GABAAandGABAA-ρReceptors 8

GABAA Receptors 8

GABAA-ρ Receptors 9

GABA Miscellaneous 9

Glutamate(Ionotropic)Receptors 9

AMPA Receptors 9

Kainate Receptors 10

NMDA Receptors 10

Other Glutamate 12

GlycineReceptors 13

HCNChannels 13

IP3Receptors 13

Purinergic(P2X)Receptors 13

Voltage-gated Ion Channels 15

CalciumChannels 16

Ryanodine Receptors 16

STIM-Orai Channels 16

Voltage-gated Calcium Channels 16

Other Calcium Channels 17

PotassiumChannels 17

Ca2+-Activated Potassium Channels 17

Inward Rectifier Potassium (Kir) Channels 18

Two-P Potassium Channels 19

Voltage-gated Potassium (Kv) Channels 19

Non-selective / Other Potassium Channels 19

SodiumChannels 20

Voltage-gated Sodium Channels 20

TransientReceptorPotentialChannels 20

TRPA1 20

TRPC 20

TRPM 20

TRPML 21

TRPP 21

TRPV 21

The Comprehensive in Vitro Proarrhythmia 23Assay Initiative (CiPA)

Other Channels 24

Aquaporins 24

ChlorideChannels 24

Calcium-activated Chloride Channels 24

CFTR 24

Other Chloride Channels 24

Ionophores 24

PhotoswitchableLigands 25

OtherChannelModulators 25

Antibodies Targeting Ion Channels 26

References 27

Ion channeLS

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GRIN1

GRIN3B

GRIN3A

GLRA3

GLRA1

GLRA2GLRA4

GLRBGABRR2

GABRR1GABRR3

GABRP

GABRD

GABRB3

GABRB2

GABRB1

GABRQ

GABRG2

GABRG1

GABRG3GABRE

GABRA6

GABRA4

GABRA2

GABRA1GABRA5GABRA3

CHRNA1

HTR3A HTR3B HTR3D

HTR3CHTR3ECHRNA2CHRNA4

CHRNA3CHRNA6

CHRNA

CHRNB3CHRNB2CHRNB4

CHRNB1CHRND

CHRNECHRNG

CHRNA7

CHRNA10

CHRNA9

GRIA3GRIA1

GRIA2

GRIA4

GRIK2

GRIK1

GRIK3GRIK4

GRIK5

GRIN2D

GRIN2C

GRIN2B

GRIN2A

P2XENaC

ASIC

NMDA

Kainate

AMPA

nAChR

5-HT

GlyR

GABAa

P2RX3

P2RX2 P2RX4

P2RX1

P2RX5

P2RX6

P2RX7

SCNN1A SCNN1D

SCNN1B

SCNN1G

ASIC2

ASIC1

ASIC3

ASIC4

ASIC5

Figure 1 | A representation of the ligand-gated ion channel gene tree featuring genes of ion channels targeted by tocris products

Ligand-gated Ion channelsLigand-gated ion channels are a large group of transmembrane proteins that allow the passage of ions through the membrane in response to the binding of a specific chemical messenger; they are also known as ionotropic receptors. Ligand-gated ion channels are grouped according to the endogenous compound to which they selectively respond; these include 5-HT, ATP, GABA, glutamate, acetylcholine and glycine. In general, the binding site for the ligand is distinct from the pore, and binding results in either channel opening or closing.

Gene abbreviation

Ion Channel

ASIC acid-sensing ion channelCHRNA cholinergic receptor nicotinic alpha subunit CHRNB cholinergic receptor nicotinic beta subunit CHRND cholinergic receptor nicotinic delta subunit CHRNE cholinergic receptor nicotinic epsilon subunit CHRNG cholinergic receptor nicotinic gamma subunit GABRA γ-aminobutyric acid type a receptor alpha subunitGABRB γ-aminobutyric acid type a receptor beta subunitGABRD γ-aminobutyric acid type a receptor delta subunitGABRE γ-aminobutyric acid type a receptor epsilon

subunitGABRG γ-aminobutyric acid type a receptor gamma

subunitGABRP γ-aminobutyric acid type a receptor pi subunitGABRQ γ-aminobutyric acid type a receptor theta subunitGABRR γ-aminobutyric acid type a receptor rho subunitGRIA glutamate ionotropic receptor aMPa type subunitGRIK glutamate ionotropic receptor kainate type

subunitGRIN glutamate ionotropic receptor nMDa type subunitGLRA glycine receptor alphaGLRB glycine receptor betaHTR3 5-hydroxytryptamine receptor 3P2RX purinergic receptor P2XSCNN sodium channel epithelial (enac)

adapted from www.guidetopharmacology.org


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5-HT3

Agonists 0440 m-chlorophenylbiguanide Potent and specific 5-hT3 agonist 100 mg

0558 2-Methyl-5-hydroxytryptamine 5-hT3 agonist/potent 5-hT6 ligand 10 mg

50 mg

0566 N-Methylquipazine 5-hT3 agonist 100 mg

0629 Quipazine 5-hT3 agonist 100 mg

0988 RS 56812 5-hT3 partial agonist 10 mg

50 mg

3547 Serotonin endogenous 5-hT receptor agonist 50 mg

1205 SR 57227 Potent, selective 5-hT3 agonist 10 mg

50 mg

Antagonists 0666 3-aQc 5-hT3 antagonist 10 mg

50 mg

2759 B-hT 920 5-hT3 antagonist; also α2 agonist and D2 receptor agonist 10 mg

50 mg

0475 Dihydroergotamine non-selective 5-hT antagonist; also partial α agonist 100 mg

5629 Dolasetron Potent and selective 5-hT3 antagonist 10 mg

50 mg

2903 Granisetron 5-hT3 antagonist 10 mg

50 mg

0640 MDL 72222 5-hT3 antagonist 50 mg

2018 Mirtazapine 5-hT3, 5-hT2, h1 and α2-antagonist; antidepressant 10 mg

50 mg

2844 Mosapride citrate 5-hT3 antagonist and 5-hT4 agonist 10 mg

50 mg

2891 ondansetron Selective 5-hT3 antagonist 10 mg

50 mg

2037 SDZ 205-557 5-hT3 and 5-hT4 receptor antagonist 10 mg

50 mg

0641 Tropanyl-3,5-dimethylbenzoate 5-hT3 antagonist 100 mg

2459 Tropisetron Potent 5-hT3 receptor antagonist; also partial agonist of α7 nachR 10 mg

50 mg

4532 VUF 10166 high affinity 5-hT3 receptor antagonist 10 mg

50 mg

0380 Y-25130 Potent, selective 5-hT3 antagonist 10 mg

50 mg

1795 Zacopride highly potent 5-hT3 receptor antagonist; also 5-hT4 agonist 10 mg

50 mg

AcetylcholineNicotinicReceptorsnicotinic (α7) Receptors

Agonists 4234 4BP-TQS allosteric agonist at α7 nachR 10 mg

4341 a 582941 Partial agonist at α7 nachR 10 mg

50 mg

4477 a 844606 Selective α7 nachR partial agonist 10 mg

50 mg

2809 acetylcholine endogenous neurotransmitter 50 mg

3964 aR-R 17779 α7-selective agonist 10 mg

2241 DMaB-anabaseine Partial agonist at α7 nachR; also α4β2 antagonist 10 mg

50 mg

4557 GTS 21 Partial agonist at α7 nachR 10 mg

50 mg

3092 Pha 543613 Potent and selective α7 nachR agonist 10 mg

3134 Pha 568487 α7-selective agonist 10 mg

50 mg

2303 PnU 282987 Selective α7 nachR agonist 10 mg

50 mg

Category Cat. no. Product name Description Unit size

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1271 RJR 2429 nicotinic receptor agonist 10 mg

50 mg

3518 S 24795 Partial agonist at α7 nachR 10 mg

50 mg

4441 Sen 12333 α7 nachR agonist; histamine h3 antagonist 10 mg

50 mg

5559 SSR 180711 Partial agonist at α7 nachR 10 mg

50 mg

2518 Tc 1698 α7-selective agonist 10 mg

50 mg

Antagonists 2133 α-Bungarotoxin α7 subtype-selective nachR antagonist 1 mg

3119 α-conotoxin ImI α7 and α9 selective nachR antagonist 500 μg

3405 coG 133 nicotinic α7 antagonist; apoe peptide fragment 1 mg

1029 Methyllycaconitine α7 neuronal nicotinic receptor antagonist 5 mg

25 mg

1356 MG 624 α7 neuronal nicotinic receptor antagonist 10 mg

50 mg

Modulators 4571 a 867744 Positive allosteric modulator of α7 nachR 10 mg

50 mg

3837 ccMI Positive allosteric modulator of α7 nachR 10 mg

50 mg

1260 Ivermectin allosteric modulator of α7 nicotinic receptors 100 mg

Ligand-gated Ion channels – continued

Immunology feature products

NN

N

N Cl

Cl

N

A 438079 (2972)Competitive P2X7 receptor antagonist

HNO

HN

OHN

O

HN

O

HN

SO3Na

SO3Na

NaO3S

NaO3S

NaO3S

NaO3S

OHN

NaO3S

NaO3S

NF 449 (1391)Potent and selective P2X1

receptor antagonist

NN

Cl

TRAM 34 (2946)Potent and highly selective KCa3.1

channel blocker

O

OMeN

N

OMe

SKF 96365 (1147)Inhibits STIM1-mediated Ca2+

influx; also TRPC channel inhibitor

OH

NH

NH

SO

O

5J 4 (5490)CRAC channel blocker; blocks store-operated calcium entry

P2X7 receptors expressed on T cells and microglia are associated with cell migration, proliferation, and cytokine release as well as

Th17 differentiation.Calcium is a second messenger in

lymphocytes, regulating proliferation, gene expression, motility and other functions. STIM1 is the putative Ca2+ sensor on the

endoplasmic reticulum (ER).

Potassium channels regulate the membrane potential of lymphocytes and KCa3.1

channels are associated with membrane hyperpolarization in response to elevated

intracellular Ca2+ levels.

CRAC channels are expressed in lymphocytes and are activated in response

to depleted intracellular Ca2+ stores. Ca2+ release from ER is triggered by IP3 in response to antigen receptor activation.

P2X1 receptors are expressed on T cells and are associated activation.

Ion Channels in Immunology Research T and B cells and microglia express a wide variety of ion channels, which are implicated in immune processes. Below is a selection of compounds from Tocris that may be used to explore the role of ion channels in the immune system.



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4141 LY 2087101 Potentiator of α7 nachRs 10 mg

50 mg

2995 nS 1738 Positive allosteric modulator of α7 nachR; active in vivo 10 mg

50 mg

2498 PnU 120596 Positive allosteric modulator of α7 nachR; active in vivo 10 mg

50 mg

4233 TQS Positive allosteric modulator of α7 nachRs 10 mg

50 mg

Other 5156 Ivermectin B1a-d2 Deuterated ivermectin B1a (cat. no. 1260) 1 mg

nicotinic (α4β2) receptors

Agonists 5017 a 85380 high affinity and selective α4β2 agonist 10 mg

5079 aBT 089 high affinity and selective α4β2 partial agonist 10 mg

50 mg

5236 cc4 high affinity and subtype-selective α6β2 and α4β2 partial agonist 10 mg

50 mg

4125 3-pyr-cytisine high affinity, partial agonist of α4β2 receptors 10 mg

50 mg

5557 Dianicline Selective α4β2 nachR partial agonist 10 mg

50 mg

1518 5-Iodo-a-85380 high affinity α4β2 and α6β2 subtype-selective agonist 10 mg

1527 5-Iodo-a-85380, 5-trimethylstannyl n-Boc derivative

Precursor to 5-Iodo-a-85380 (cat. no. 1518) 200 μg

1053 RJR 2403 α4β2 selective nicotinic agonist 10 mg

50 mg

2737 Tc 2559 Selective partial agonist at α4β2 receptors 10 mg

50 mg

3754 Varenicline orally active, subtype-selective α4β2 partial agonist 10 mg

50 mg

2nd agonist/competitive antagonist site

Agonist/competitive antagonist binding siteat subunit interface

M2 lines the cation channel

Subunit topographyPentameric nAChR with central cation channel and notional sites for drug interactions

Allosteric modulator sites

Channel blocker/non-competitive antagonist

Ca2+, Na+

K+

Out

In

M1 M2 M3 M4

C

N

Cys-loop

ACh binding protein (AChBP)

CC


Left: The topography of a single nachR subunit. The two cysteine residues forming the signature cys-loop are indicated. The extracellular n-terminal domain corresponds to the achBP. Right: Schematic of a generic nachR showing 5 subunits spanning the membrane to form a central ion channel. notional sites of action of interacting drugs are shown: two agonist binding sites are indicated at extracellular subunit interfaces, consistent with a heteromeric nachR. competitive antagonist sites overlap the agonist binding sites. extracellular and intramembrane sites have been proposed for different allosteric modulators. non-competitive antagonists may occlude or block the ion channel, as indicated, or may act at other sites. See text for further details.

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Modulators 3328 Desformylflustrabromine Positive allosteric modulator of α4β2; also muscle-type nachR inhibitor

10 mg

50 mg

5112 nS 9283 Positive allosteric modulator of α4β2 10 mg

50 mg

Other 2736 Sazetidine a α4β2 receptor ligand; may act as an agonist or a desensitizer 10 mg

nicotinic Receptors (non-selective/other)

Agonists 0351 1-acetyl-4-methylpiperazine nicotinic agonist 10 mg

50 mg

0352 4-acetyl-1,1-dimethylpiperazinium nicotinic agonist 10 mg

50 mg

1971 (+)-anabasine neuronal nicotinic receptor partial agonist 50 mg

0789 (±)-anatoxin a nicotinic agonist 1 mg

3549 3-Bromocytisine Potent agonist of α4β4, α4β2 and α7 nach receptors 10 mg

50 mg

2810 carbamoylcholine cholinergic receptor agonist 100 mg

3110 (-)-cotinine Major metabolite of nicotine 50 mg

1390 (-)-cytisine Potent, selective neuronal nicotinic agonist 10 mg

50 mg

0684 (±)-epibatidine high affinity nicotinic agonist 10 mg

1077 (-)-Lobeline nicotinic partial agonist 100 mg

3546 (-)-nicotine Prototypical nachR agonist 50 mg

4831 nS 3861 α3β2 full agonist; also α3β4 partial agonist 10 mg

50 mg

3855 RuBi-nicotine caged nicotine; rapidly excitable by visible light 10 mg

4766 SIB 1508Y Potent agonist of α4β2, α2β4, α4β4 and α3β4 nach receptors 10 mg

50 mg

4764 SIB 1553a Subunit selective nachR agonist 10 mg

50 mg

1348 UB 165 Subunit selective nachR agonist 10 mg

Antagonists 3205 acV 1 α9α10-selective antagonist 100 μg

4128 Bisindolylmaleimide II nicotinic receptor antagonist; also potent PKc inhibitor 10 mg

50 mg


Human α4β2 nicotinic ReceptorX-Ray crystal structure of α4β2 nicotinic receptor in complex with nicotine

Image adapted from RScB Protein Data Bank (http://www.rcsb.org). PDB ID: 5KXI Morales-Perez et al. (2016) Nature 538 411. PMID 27698419.

• Nicotine is the prototypical nAChR agonist (Ki = 1 nM)

• The effects of nicotine in the brain, including its reinforcing properties that lead to addiction, are mediated by α4β2 receptors

• Nicotine binds in the classical neurotransmitter site at the α–β interface.

Cat. No. 3546N

N

Cat. No. 3546

Cat. No. 2555O

MeHN

.HCI

O

ON

N

O


http://www.rcsb.org/


8 |

0424 Benzoquinonium nicotinic antagonist 10 mg

50 mg

3221 bPiDDB orthosteric nachR antagonist 10 mg

50 mg

2722 catestatin non-competitive nicotinic cholinergic antagonist 1 mg

1001 chlorisondamine nicotinic antagonist; slow offset 10 mg

50 mg

3120 α-conotoxin auIB Selective α3β4 nachR antagonist 500 μg

3124 α-conotoxin eI α1β1δγ selective nachR antagonist 500 μg

1340 α-conotoxin MII Potent α3β2 and β3 subunit selective nicotinic antagonist 500 μg

3121 α-conotoxin PIa Selective antagonist of α6-containing nicotinic receptors 500 μg

3123 α-conotoxin PnIa Selective α3β2 nachR antagonist 500 μg

2349 Dihydro-β-erythroidine antagonist for neuronal α4-containing nicotinic receptors 10 mg

50 mg

4111 hexamethonium nicotinic receptor blocker 50 mg

2843 Mecamylamine non-competitive nicotinic receptor antagonist 10 mg

50 mg

0693 Pancuronium nicotinic (neuromuscular) antagonist 10 mg

50 mg

4424 SR 16584 Selective α3β4 nachR antagonist 10 mg

50 mg

2438 TMPh neuronal nicotinic receptor antagonist 10 mg

50 mg

2820 (+)-Tubocurarine nicotinic receptor antagonist 50 mg

Other 0686 Galanthamine neuronal nicotinic receptor potentiator; also cholinesterase inhibitor 100 mg

Acid-SensingIonChannelsActivators 5028 GMQ Selective aSIc3 opener 10 mg

50 mg

Blockers 4804 aPeTx2 aSIc3 channel blocker 100 μg

5938 Mambalgin 1 Selective aSIc1a inhibitor; analgesic 10 μg

5042 Psalmotoxin 1 Potent and selective aSIc1a channel blocker 100 μg

EpithelialSodiumChannelsActivators 0464 capsazepine activator of enacδ; also vanilloid receptor antagonist 10 mg

50 mg

Blockers 3380 Benzamil Deg/enac channel blocker; amiloride (cat. no. 0890) derivative; also ncX inhibitor

10 mg

50 mg

GABAAandGABAA-ρReceptorsGABAA Receptors

Agonists 0289 Muscimol Potent GaBaa agonist 1 mg

10 mg

50 mg

0807 ThIP GaBaa agonist; also GaBaa -ρ antagonist 50 mg

Antagonists 2503 (-)-Bicuculline methiodide Water-soluble GaBaa antagonist 10 mg

50 mg

0109 (-)-Bicuculline methobromide Water-soluble GaBaa antagonist 10 mg

50 mg

0131 (-)-Bicuculline methochloride Water-soluble GaBaa antagonist 10 mg

50 mg

0130 (+)-Bicuculline Potent GaBaa antagonist 50 mg

1128 Picrotoxin GaBaa receptor antagonist 1 g

1262 SR 95531 Selective, competitive GaBaa receptor antagonist 10 mg

50 mg

Benzodiazepines 5281 ac 5216 Selective TSPo ligand 10 mg

50 mg

1327 L-655,708 Benzodiazepine inverse agonist; selective for α5-containing GaBaa receptors

10 mg

50 mg


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2832 Midazolam Benzodiazepine agonist 10 mg

50 mg

0670 PK 11195 antagonist at peripheral benzodiazepine receptors 10 mg

50 mg

0655 Zolpidem Benzodiazepine agonist 10 mg

50 mg

Modulators 3653 allopregnanolone GaBaa receptor positive allosteric modulator 10 mg

3113 etifoxine Potentiator of GaBaa receptors; anxiolytic 10 mg

50 mg

1471 etomidate GaBa mimetic and GaBa modulatory agent 10 mg

50 mg

2531 Ganaxolone Potent, positive allosteric modulator of GaBaa receptors 10 mg

50 mg

3652 Pregnanolone GaBaa receptor positive allosteric modulator 50 mg

GABAA-ρ Receptors

Agonists 0379 SKF 97541 GaBaa-ρ antagonist; also extremely potent GaBaB agonist 10 mg

50 mg

0180 ZaPa agonist at ‘low affinity’ GaBaa receptor; more potent than GaBa/muscimol

10 mg

50 mg

Antagonists 1040 TPMPa Selective GaBaa-ρ antagonist 10 mg

50 mg

GABA Miscellaneous

Other 2991 DPnI-caged-GaBa nitroindoline-caged GaBa 10 mg

2687 Pentylenetetrazole convulsant 1 g

3400 RuBi-GaBa caged GaBa; excitable by visible wavelength 10 mg

Glutamate(Ionotropic)ReceptorsAMPA Receptors

Antagonists 2555 GYKI 53655 non-competitive aMPa receptor antagonist 10 mg

50 mg

1636 IeM 1460 open-channel blocker of aMPa currents; selective for non-GluR2-containing receptors

10 mg

50 mg

2345 ZK 200775 competitive aMPa/kainate antagonist 10 mg

50 mg


AMPA-subtype Ionotropic Glutamate ReceptorX-Ray crystal structure of rat GluA2 receptor in complex with the noncompetitive inhibitor GYKI 53655

Image adapted from RScB Protein Data Bank (http://www.rcsb.org). PDB ID: 5L1h Yelshanskaya et al. (2016) Neuron 91 1305. PMID 27618672

• GYKI 53655 is a non-competitive AMPA and kainate receptor antagonist. IC50 is 18.9 μM for AMPA receptors.

• GYKI 53655 exhibits anticonvulsant activity.

• The compound binds at the interface between the ion channel and the linkers connecting the transmembrane domain and the ligand-binding domain.

Cat. No. 2555

N

N

Cat. No. 3546

Cat. No. 2555O

MeHN

.HCI

O

ON

N

O


http://www.rcsb.org/


10 |

Other 6094 2R,6R-hydroxynorketamine enhances aMPa currents; metabolite of Ketamine (cat. no. 3131) 10 mg

6095 2S,6S-hydroxynorketamine enhances aMPa currents; metabolite of Ketamine (cat. no. 3131) 10 mg

5982 cis-6-hydroxynorketamine enhances aMPa currents; metabolite of Ketamine (cat. no. 3131) 10 mg

50 mg

Kainate Receptors

Agonists 0269 Domoic acid Potent, selective kainate agonist 1 mg

5 mg

0222 Kainic acid Potent excitant and neurotoxin 1 mg

10 mg

50 mg

Antagonists 2728 aceT Potent antagonist of GluR5-containing kainate receptors 10 mg

0190 cnQX Potent aMPa/kainate antagonist 10 mg

50 mg

1045 cnQX disodium salt Potent aMPa/kainate antagonist; more water soluble form of cnQX (cat. no. 0190)

1 mg

10 mg

50 mg

0189 DnQX Selective non-nMDa antagonist 10 mg

50 mg

2312 DnQX disodium salt Selective non-nMDa antagonist; water-soluble salt of DnQX (cat. no. 0189)

10 mg

50 mg

3620 Topiramate GluR5 antagonist; inhibits carbonic anhydrase (ca) II and IV 10 mg

50 mg

2079 UBP 302 Potent and selective kainate antagonist; active enantiomer of UBP 296 (cat. no. 2078)

10 mg

50 mg

nMDA Receptors

Agonists 0186 cis-acPD Potent nMDa agonist; also group II mGluR agonist 10 mg

50 mg

0213 d-aspartic acid nMDa agonist 1 g

0214 l-aspartic acid nMDa agonist 1 g

0216 l-cysteinesulfinic acid nMDa and mGlu agonist 100 mg

3406 GLYX 13 nMDa receptor partial agonist; acts at the glycine site 1 mg

0197 homoquinolinic acid Selective, potent nMDa agonist 10 mg

50 mg

0285 Ibotenic acid non-selective nMDa agonist 5 mg

2277 MnI-caged-d-aspartate caged d-aspartate; nMDa agonist 10 mg

50 mg

0114 nMDa Selective nMDa agonist 50 mg

500 mg

0225 Quinolinic acid endogenous nMDa agonist and transmitter candidate 1 g

0959 Spermidine tri agonist at polyamine site of nMDa receptor 100 mg

0312 (RS)-(Tetrazol-5-yl)glycine highly potent nMDa receptor agonist 10 mg

50 mg

Antagonists 0106 d-aP5 Potent, selective nMDa antagonist; more active form of dl-aP5 (cat. no. 0105)

1 mg

10 mg

50 mg

100 mg

0105 dl-aP5 Potent, selective nMDa antagonist 10 mg

50 mg

3693 dl-aP5 sodium salt nMDa antagonist; sodium salt of dl-aP5 (cat. no. 0105) 10 mg

50 mg

0104 dl-aP7 Selective nMDa antagonist 10 mg

50 mg

0107 l-aP5 Potent, selective nMDa antagonist; less active form of dl-aP5 (cat. no. 0105)

10 mg

50 mg

1469 cGP 37849 Potent and selective nMDa antagonist 10 mg

50 mg


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1409 cGP 39551 Potent, selective and competitive nMDa antagonist 10 mg

50 mg

1493 cGP 78608 Potent, selective glycine-site nMDa antagonist 10 mg

50 mg

1241 cGS 19755 Potent, competitive nMDa antagonist 10 mg

50 mg

0237 7-chlorokynurenic acid nMDa receptor antagonist; also potent competitive inhibitor of l-glutamate uptake

10 mg

50 mg

3697 7-chlorokynurenic acid sodium salt nMDa antagonist; also potent competitive inhibitor of L-glutamate uptake; sodium salt of 7-chlorokynurenic acid (cat. no. 0237)

10 mg

50 mg

2456 co 101244 highly selective nR2B antagonist 10 mg

50 mg

4136 conantokin G nR2B-selective nMDa receptor antagonist 500 μg

3125 conantokin-R Potent non-competitive nMDa receptor antagonist 500 μg

3122 conantokin-T non-competitive nMDa receptor antagonist 500 μg

0247 (R)-cPP Potent nMDa antagonist; more active enantiomer of (RS)-cPP (cat. no. 0173)

10 mg

50 mg

0173 (RS)-cPP Potent nMDa antagonist 10 mg

50 mg

1265 d-cPP-ene Potent, competitive nMDa antagonist 10 mg

0286 5,7-Dichlorokynurenic acid Potent nMDa antagonist, acts at glycine site 10 mg

50 mg

3698 5,7-Dichlorokynurenic acid sodium salt Potent nMDa antagonist, acts at glycine site; sodium salt of 5,7-Dichlorokynurenic acid (cat. no. 0286);

10 mg

50 mg

0360 (±)-1-(1,2-Diphenylethyl)piperidine nMDa antagonist, acts at ion channel site 10 mg

50 mg

4491 DQP 1105 Selective nR2c/nR2D receptor antagonist 10 mg

50 mg

2195 eliprodil non-competitive nR2B-selective nMDa antagonist 10 mg

50 mg

2348 Gavestinel Potent and selective glycine site antagonist; orally available and active in vivo

10 mg

50 mg

0545 Ifenprodil non-competitive nMDa antagonist; also σ ligand 10 mg

50 mg

3131 Ketamine non-competitive nMDa receptor antagonist 50 mg

4379 (S)-(+)-Ketamine nMDa receptor antagonist; enantiomer of ketamine (cat. no. 3131) 50 mg

0742 L-689,560 Very potent nMDa antagonist 10 mg

50 mg

1019 LY 235959 competitive nMDa antagonist 10 mg

50 mg

0773 Memantine nMDa antagonist; acts at ion channel site 50 mg

0924 (+)-MK 801 maleate non-competitive nMDa antagonist; acts at ion channel site 10 mg

50 mg

0955 (-)-MK 801 maleate nMDa antagonist, less active enantiomer 10 mg

50 mg

1970 norketamine Potent, non-competitive nMDa antagonist 10 mg

50 mg

5018 PeaQX tetrasodium salt Potent nMDa receptor antagonist; nR2a selective 10 mg

2557 Phencyclidine non-competitive nMDa receptor antagonist 10 mg

50 mg

2530 PPDa Subtype-selective nR2c/nR2D antagonist 10 mg

50 mg

2274 PPPa competitive nR2a antagonist 10 mg

50 mg

4801 QnZ 46 nR2c/nR2D-selective nMDa receptor non-competitive antagonist 10 mg

50 mg




12 |

2005 Ro 04-5595 nR2B-selective nMDa antagonist 10 mg

50 mg


10 mg

50 mg


50 mg

1250 SDZ 220-581 competitive nMDa antagonist 10 mg

50 mg

4154 Tcn 201 Selective nR1/nR2a receptor antagonist 10 mg

50 mg

4163 Tcn 213 nMDa antagonist; selective for nR2a over nR2B 10 mg

50 mg

4072 Tcn 237 highly potent and selective nR2B antagonist 10 mg

2782 TcS 46b orally active, subtype-selective nR1a/nR2B antagonist 10 mg

50 mg

2892 Threo Ifenprodil nR2B-selective nMDa antagonist; also σ agonist 10 mg

50 mg

3322 ZD 9379 Brain penetrant nMDa antagonist; acts at glycine site 10 mg

Other 4105 cIQ Potentiator of nMDa receptors containing nR2c/nR2D 10 mg

50 mg

0226 d-Serine nMDa potentiator; acts at glycine site 1 g

2224 MnI-caged-nMDa caged nMDa 10 mg

2213 n20c non-competitive nMDa receptor open-channel blocker 10 mg

50 mg

5996 R-norketamine nMDa receptor modulator; metabolite of Ketamine (cat. no. 3131) 10 mg

6112 S-norketamine nMDa receptor modulator; metabolite of Ketamine (cat. no. 3131) 10 mg

4230 nPec-caged-d-aP5 caged d-aP5 (cat.no. 0106) 10 mg

50 mg

5376 Pregnenolone sulfate sodium salt nMDa Potentiator 50 mg

0958 Spermine Modulator at polyamine site on nMDa receptors 100 mg

other Glutamate

Agonists 0217 d-Glutamic acid endogenous, non-selective agonist; less active enantiomer 1 g

0218 l-Glutamic acid endogenous, non-selective agonist 1 g

0391 Spaglumic acid Weak activator of nMDa receptors; also selective mGlu3 agonist 50 mg

Antagonists 0102 d-aP4 Broad spectrum eaa antagonist 10 mg

50 mg

0101 dl-aP4 Broad spectrum eaa antagonist 100 mg

3699 dl-aP4 Sodium salt Broad spectrum eaa antagonist; sodium salt of DL-aP4 (cat. no. 0101)

50 mg

0341 l-aP6 Selective agonist of the ‘quis’ effect 10 mg

50 mg

2538 l-BMaa neurotoxic amino acid 10 mg

0321 (RS)-4-carboxyphenylglycine Broad spectrum eaa ligand 10 mg

50 mg

0310 (RS)-4-carboxy-3-hydroxyphenylglycine Broad spectrum eaa ligand 10 mg

50 mg

0328 (R)-3-carboxy-4-hydroxyphenylglycine Ionotropic glutamate receptor antagonist 10 mg

50 mg

1395 (R)-3,4-DcPG aMPa antagonist; weak nMDa antagonist 10 mg

50 mg

1394 (RS)-3,4-DcPG Potent systemically active anticonvulsant. Racemate of (R)-3,4,-DcPG (cat. no. 1395)

10 mg

50 mg

0112 γDGG Broad spectrum glutamate receptor antagonist 50 mg

0223 Kynurenic acid Broad spectrum eaa antagonist 1 g

3694 Kynurenic acid sodium salt Sodium salt of kynurenic acid (cat. no. 0223) 100 mg


Ion channeLS

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Other 5785 MDnI-caged-l-glutamate Stable photoreleaser of l-glutamate 10 mg

1490 MnI-caged-l-glutamate Stable photoreleaser of l-glutamate 10 mg

50 mg

0395 n-acetylglycyl-d-glutamic acid Potent convulsant 10 mg

50 mg

3574 RuBi-Glutamate caged glutamate; excited by visible wavelengths 10 mg

0636 Salsolinol-1-carboxylic acid endogenous amino acid 10 mg

50 mg

3847 Theanine Glutamate receptor ligand 50 mg

GlycineReceptorsAgonists 0206 β-alanine endogenous glycine agonist; more selective than taurine

(cat. no. 0209)1 g

0205 L-alanine Glycine receptor agonist 1 g

0219 Glycine endogenous glycine agonist; also modulates nMDa receptor-mediated neurotransmission

1 g

0208 hypotaurine non-selective endogenous glycine receptor agonist 100 mg

0227 L-Serine Weak endogenous glycine receptor agonist 1 g

0209 Taurine non-selective, endogenous glycine receptor partial agonist 1 g

HCNChannelsBlockers 2202 Zatebradine Blocks hyperpolarization-activated current (If) 10 mg

50 mg

1000 ZD 7288 Inhibits pacemaker (If) current 10 mg

50 mg

IP3ReceptorsAntagonists 1224 2-aPB IP3 receptor antagonist; also TRP channel modulator 10 mg

50 mg

1280 (-)-Xestospongin c Reported inhibitor of IP3-dependent ca2+ release 10 μg

Other 6210 ci-IP3/PM caged inositol triphosphate 10 μg

Purinergic(P2X)ReceptorsAgonists 3245 aTP P2 agonist 50 mg

4080 aTPγS P2 agonist; aTP (cat. no. 3245) analog 10 mg

3312 BzaTP P2X7 agonist and P2X1/P2Y1 partial agonist; also photoaffinity label for aTPase

1 mg

3209 α,β-Methyleneadenosine 5’-triphosphate P2 agonist 10 mg

1062 2-Methylthioadenosine triphosphate P2 purinergic agonist 10 mg

Antagonists 2972 a 438079 competitive P2X7 antagonist 10 mg

50 mg

3701 a 740003 Potent and selective P2X7 antagonist 10 mg

50 mg

4473 a 804598 Potent and selective P2X7 antagonist 10 mg

50 mg

4232 a 839977 Potent P2X7 antagonist 10 mg

50 mg

3323 aZ 10606120 Potent P2X7 receptor antagonist 10 mg

50 mg

3317 aZ 11645373 Potent and selective human P2X7 antagonist 10 mg

50 mg

3579 5-BDBD Potent P2X4 receptor antagonist 10 mg

50 mg

5545 BX 430 Selective P2X4 allosteric antagonist 10 mg

50 mg

0845 evans Blue Selective P2X purinergic antagonist; also potent inhibitor of l-glutamate uptake into synaptic vesicles

1 g

0683 iso-PPaDS P2X antagonist 10 mg

50 mg

5299 JnJ 47965567 Potent and selective P2X7 antagonist; brain penetrant 10 mg

50 mg




14 |

1277 Kn-62 non-competitive P2X7 antagonist 1 mg

1240 nF 023 Selective, competitive P2X1 antagonist 10 mg

50 mg

2548 nF 110 Potent P2X3 antagonist 10 mg

50 mg

2450 nF 157 Selective P2Y11/P2X1 antagonist 10 mg

50 mg

1199 nF 279 Potent and selective P2X1 antagonist 10 mg

50 mg

1391 nF 449 highly selective P2X1 antagonist 10 mg

50 mg

0625 PPaDS P2 purinergic antagonist 10 mg

50 mg

1309 PPnDS Potent, selective P2X1 antagonist 10 mg

50 mg

2188 Ro 0437626 Selective P2X1 antagonist 1 mg

10 mg

4391 Ro 51 Potent P2X3, P2X2/3 antagonist 10 mg

50 mg

3052 Ro-3 Selective P2X3 and P2X2/3 antagonist 10 mg

4386 Tc-P 262 Selective P2X3, P2X2/3 antagonist 10 mg

50 mg

2464 TnP-aTP Potent, selective P2X antagonist 5 mg

Modulators 3385 GW 791343 P2X7 allosteric modulator 10 mg

50 mg

Other 5157 DMnPe-caged aTP caged aTP 10 mg

1203 MRS 2219 Potentiates P2X1-mediated responses 10 mg

50 mg



New Compound Libraries

Tocris has launched a range of new compound libraries composed of biologically active molecules that have proven pharmacological activity against a wide range of targets. Use them in your phenotypic screening studies, drug repurposing campaigns or for validation of new molecular targets. compounds are supplied pre-dissolved in DMSo, and full chemical and biological data are available. all compounds have the same proven solubility, purity and stability as all those in the Tocris catalog.

Tocriscreen Plus (Cat. No. 5840)A unique library of 1280 biologically active compounds, including 177 ion channel modulators, with many exclusive to Tocris (250 mL 10 mM DMSO solutions). The collection is also available in smaller aliquots of 50 μL as the Tocriscreen Plus Mini (Cat No. 5841).

Tocriscreen Library of FDA Approved Compounds (Cat. No. 5932) A library of 160 FDA-approved compounds (250 mL 10 mM DMSO solutions)

Tocris also has a Custom Compound Library service available.

For more information visit www.tocris.com/tocriscreen

Ion channeLS

www.tocris.com | 15

Voltage-gated Ion channelsVoltage-gated ion channels are a group of transmembrane proteins that are activated by changes in membrane potential. The alteration in membrane potential induces a conformational change in the channel protein that either opens or closes the pore. Voltage-gated ion channels are important in excitable cells such as neurons and myocytes, and they are classified according to ion selectivity, including Na+, K+, Ca2+. Also included in this group are a number of ion channel types that are relatively insensitive to changes in voltage, and are gated by second messengers or other intracellular or extracellular mediators, these include TRP channels and ryanodine receptors.

SCN11A

CACNA1G

CACNA1HCACNA1I

CACNA1ECACNA1A

CACNA1B

CACNA1C

CACNA1S

CACNA1D

CACNA1F

SCN10ASCN5A

SCN4ASCN8A

SCN9A

SCN2A

SCN3ASCN1A

TRPP3

TRPP1

TRPP2

ITPR2

ITPR1

ITPR3

TRPA1 TRPV3

TRPV4

TRPV1

TRPV2TRPV5

TRPV6MCOLN1

MCOLN2

MCOLN3

TRPC1

TRPC4

TRPC2

TRPC5

TRPC7TRPC3

TRPM1

TRPM3TRPM6TRPM7

TRPM

TRPC

TRPML

K2P

TRPV

IP3

TRPP

Kir

KCa

Kv4

Kv7

Kv6

Kv9

Kv2

Kv8

Kv5

Kv3

Kv1

HCN

Kv10

ORAI

Kv11Kv12

NaV

CaV

TRPA

TRPM2

TRPM8

TRPC6

TRPM4

TRPM5

ORAI1

ORAI2

ORAI3

HCN1HCN2

KCNH1

KCNH5

KCNH7

KCNH2

KCNH6KCNH8

KCNH4

KCNH3

RYR1

RYR2

RYR3

KCNG1KCNG2

KCNG3KCNG4

KCNS3

KCNK7KCNK6

KCNK1

KCNK4

KCNK2

KCNK10KCNK5

KCNK3

KCNK9

KCNK12 KCNK13

KCNK18 KCNK18

KCNK18

KCNN4KCNN3

KCNN2

KCNU1

KCNJ15

KCNJ10KCNJ1

KCNJ8

KCNJ11KCNJ2

KCNJ12KCNJ4

KCNJ14KCNJ6

KCNJ5

KCNJ9

KCNJ3

KCNJ16

KCNJ13

KCNN1

KCNMA1KCNK16

KCNS2KCNS1

KCNB2

KCNB1

KCNV1KCNV2 KCNF1

KCNC3

KCNC4KCNC1 KCNC2

KCNA10KCNA5

KCNA6KCNA2

KCNA7KCNA1

KCNA3

KCNA4

KCND3

KCND2

KCND1

KCNQ1KCNQ2

KCNQ3KCNQ4

KCNQ5

HCN3

HCN4

Figure 2 | A representation of the voltage-gated ion channel gene tree featuring genes of ion channels targeted by tocris products

Gene abbreviation

Ion Channel

CACNA calcium voltage-gated channel subunits (caV)HCN hyperpolarization-activated cyclic nucleotide gated

potassium channelITPR IP3 receptorKCNA potassium voltage-gated channel subfamily a (Kv1)KCNB potassium voltage-gated channel subfamily B (Kv2)KCNC potassium voltage-gated channel subfamily c (Kv3)KCND potassium voltage-gated channel subfamily D (Kv4)KCNF potassium voltage-gated channel subfamily F (Kv5)KCNG potassium voltage-gated channel subfamily G (Kv6)KCNH potassium voltage-gated channel subfamily h

(Kv10, Kv11 and Kv12)KCNJ potassium voltage-gated channel subfamily J (Kir)KCNK two-pore potassium channel family (K2P)KCNMA1 potassium calcium-activated channel subfamily

M alpha 1 (Kca1.1)KCNN potassium calcium-activated channel subfamily nKCNQ potassium voltage-gated channel subfamily Q (Kv7)KCNS potassium voltage-gated channel subfamily S (Kv9)KCNU potassium calcium-activated channel subfamily U

(Kca5.1)KCNV potassium voltage-gated channel subfamily V (Kv8)

MCOLN transient receptor potential mucolipin familyORAI oRaI calcium release-activated calcium modulators RYR ryanodine receptorSCNA sodium voltage-gated channel alpha subunits (naV)TRPA transient receptor potential ankyrin family

TRPC transient receptor potential canonical familyTRPM transient receptor potential melastatin familyTRPP transient receptor potential (polycystin)/polycystic

kidney disease 2 familyTRPV transient receptor potential vanilloid family

adapted from www.guidetopharmacology.org


16 |

CalciumChannelsRyanodine Receptors

Activators 2793 caffeine Mobilizes calcium from intracellular stores; also a1 and a2B antagonist and cnS stimulant

100 mg

3905 naaDP RYR1 activator; ca2+ mobilizing agent 10 mg

1472 Suramin hexasodium salt Increases RYR open probability; also non-selective P2 antagonist 100 mg

Inhibitors 0507 Dantrolene Ryanodine receptor inhibitor; ca2+ release inhibitor 100 mg

4564 JTV 519 Ryanodine receptor (RyR) inhibitor 10 mg

50 mg

1329 Ryanodine ca2+ release inhibitor 1 mg

stIM-orai Channels

Inhibitors 5490 5J 4 cRac channel blocker; anti-inflammatory 10 mg

50 mg

0431 ML 9 STIM1-plasma membrane interaction inhibitor; also myosin light chain kinase inhibitor

10 mg

50 mg

1866 MRS 1845 Potent Soce inhibitor; blocks capacitative ca2+ entry 10 mg

50 mg

1147 SKF 96365 Inhibits store-operated ca2+ entry; also TRPc channel blocker 10 mg

50 mg

3939 YM 58483 Inhibitor of Soce in non-excitable cells 10 mg

50 mg

Voltage-gated Calcium Channels

Activators 1544 (±)-Bay K 8644 ca2+ channel activator (L-type) 10 mg

50 mg

1546 (S)-(-)-Bay K 8644 ca2+ channel activator (L-type) 10 mg

50 mg

1403 FPL 64176 Potent activator of ca2+ channels (L-type) 10 mg

50 mg

Cancer feature products

N N Me

O

HN

SMe

O O

E 4031 (1808)KV11.1 (hERG) channel blocker

Thr-Ile-Ile-Asn-Val-Lys-Cys-Thr-Ser-Pro-

Lys-Gln-Cys-Leu-Pro-Pro-Cys-Lys-Ala-Gln-

Phe-Gly-Gln-Ser-Ala-Gly-Ala-Lys-Cys-Met-

Asn-Gly-Lys-Cys-Lys-Cys-Tyr-Pro-His

Margatoxin (3563)Potent KV1.3 channel blocker

OO

NO

O

O OO

O

N

O O O

O

O O

O

O

O

O

BAPTA AM (2787)Blocks hKV1.5, hKV11.1 (hERG)

and hKV1.3 channels; also cell-permeable calcium chelator

N NHN

CF3

F3CO

S N

N

YM 58483 (3939)Store-operated Ca2+ entry (SOCE) blocker

in non-excitable cells; inhibits calcium release-activated calcium (CRAC) channels

Ion Channels in Cancer ResearchIon channels have recently emerged as playing a key role in the pathophysiology of cancer. Ion channels are present in all cancers and are involved in tumor development, proliferation, progression and invasiveness. For a comprehensive review of the role of ion channels in cancer see: Djamgoz et al. (2014) Philos.Trans.R.Soc.B.Biol.Sci. 369 (theme issue). Below is a selection of Tocris compounds that may be of use for exploring the role of ion channels in cancer.


Ion channeLS

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Blockers 2799 ω-agatoxin IVa ca2+ channel blocker (P-type) 10 μg

2802 ω-agatoxin TK ca2+ channel blocker (P/Q-type) 10 μg

1085 ω-conotoxin GVIa ca2+ channel blocker (n-type) 250 μg

1084 ω-conotoxin MVIIc ca2+ channel blocker (n, P and Q-type) 100 μg

2004 Isradipine ca2+ channel blocker (L-type) 10 mg

50 mg

2198 Mibefradil ca2+ channel blocker (T-type) 10 mg

50 mg

4507 ML 218 ca2+ channel blocker (T-type) 10 mg

50 mg

5711 nilvadipine ca2+ channel blocker (L-type); also Syk kinase inhibitor 50 mg

0600 nimodipine ca2+ channel blocker (L-type) 100 mg

2268 nnc 55-0396 highly selective ca2+ channel blocker (T-type) 10 mg

4665 ProTx I caV3.1 channel blocker; also inhibits naV1.8 and KV2.1 100 μg

2945 SnX 482 Potent and selective caV2.3 blocker (R-type) 10 μg

Others 0806 Gabapentin Selectively binds the α2δ subunit of caV channels. 10 mg

50 mg

3775 Pregabalin Selectively binds the α2δ subunit of voltage-sensitive calcium channels; anticonvulsant

10 mg

50 mg

other Calcium Channels

Activators 5586 Yoda 1 Piezo1 channel activator 10 mg

50 mg

4741 Gadolinium chloride Stretch-activated calcium channel blocker; calcium-sensing receptor agonist

50 mg

PotassiumChannelsCa2+-Activated Potassium Channels

Activators 2665 BMS 191011 Potent BKca (Kca1.1) channel opener 10 mg

50 mg

2953 cyPPa activator of Kca2.2 and Kca2.3 channels 10 mg

50 mg

1041 1-eBIo activator of epithelial Kca channels 10 mg

50 mg

4311 GW 542573X Selective activator of Kca2.1 channels 10 mg

50 mg

4788 nS 11021 activator of BKca (Kca1.1) channels 10 mg

50 mg



50 mg

3895 nS 309 Positive modulator of Kca2 and Kca3.1 channels 10 mg

50 mg

3670 SKa 31 activator of Kca3.1 and Kca2 channels 10 mg

50 mg

Blockers 1652 apamin Kca2 channel blocker (small conductance) 1 mg

1087 charybdotoxin Kca channel blocker (big conductance) 10 μg

1086 Iberiotoxin Kca channel blocker (big conductance) 100 μg

5571 Lei-Dab 7 high affinity, selective Kca2.2 blocker 100 μg

4864 nS 6180 Potent Kca3.1 channel blocker 10 mg

50 mg

2006 Paxilline Potent BKca channel blocker; also SeRca aTPase blocker. 10 mg

4617 Penitrem a Potent and selective BKca (Kca1.1) channel blocker 1 mg

2946 TRaM 34 Potent and highly selective Kca3.1 channel blocker 10 mg

50 mg

4952 TRaM 39 Potent Kca3.1 blocker 10 mg

50 mg

Voltage-gated Ion channels – continued



18 |

1310 UcL 1684 highly potent blocker of Kca2 5 mg

2661 UcL 2077 Slow afterhyperpolarization (sahP) channel blocker; sub-type selective Kv channel effects

10 mg

50 mg

Modulators 4597 nS 8593 Selective Kca2 (SK) channel negative modulator; inhibits SK currents 10 mg

50 mg

Inward Rectifier Potassium (Kir) Channels

Activators 1377 cromakalim Kir6 (KaTP) channel opener 10 mg

50 mg

0964 Diazoxide Kir6 (KaTP) channel opener; blocks desensitization of aMPa receptors 100 mg

1378 Levcromakalim Kir6 (KaTP) channel opener; active enantiomer of cromakalim (cat. no. 1377)

10 mg

50 mg

0583 Minoxidil Kir6 channel (KaTP) opener 100 mg

5380 ML 297 Selective Kir3.1/3.2 (GIRK1/2) channel activator 10 mg

50 mg

2147 nicorandil Kir6 (KaTP) channel opener and no donor 50 mg

1355 P1075 Potent Kir6 (KaTP) channel opener 10 mg

50 mg

2580 Tenidap opener of Kir2.3; also nSaID, cyclooxygenase (coX-1) inhibitor 10 mg

50 mg

2076 Y-26763 Kir6 (KaTP) channel opener 10 mg

50 mg

2077 Y-27152 Prodrug of Kir6 (KaTP) channel opener Y-26763 (cat. no. 2076); orally active in vivo

10 mg

50 mg

0882 ZM 226600 Kir6 (KaTP) channel opener 10 mg

50 mg

Blockers 3590 Gambogic acid Kir2.1 channel blocker; also activates caspases and inhibits Bcl-2 family proteins

10 mg

50 mg

0911 Glibenclamide Kir6 (KaTP) channel blocker 100 mg

2396 Glimepiride Kir6 (KaTP) channel blocker 10 mg

50 mg

4549 ML 133 Kir2 channel blocker 10 mg

50 mg

Venoms feature products

Leu-Lys-Cys-Tyr-Gln-His-Gly-Lys-Val-Val-

Thr-Cys-His-Arg-Asp-Met-Lys-Phe-Cys-Tyr-

His-Asn-Thr-Gly-Met-Pro-Phe-Arg-Asn-Leu-

Lys-Leu-Ile-Leu-Gln-Gly-Cys-Ser-Ser-Ser-

Cys-Ser-Glu-Thr-Glu-Asn-Asn-Lys-Cys-Cys-

Ser-Thr-Asp-Arg-Cys-Asn-Lys

Mambalgin 1 (5938)Selective ASIC1a inhibitor

Dendroaspis polylepsis, the Black Mamba, a source of Mambalgin 1

Venoms Venoms contain peptide toxins that are injected by an animal, via biting or stinging, into its prey. A variety of animals produce venoms, including snakes, spiders, cone snails, scorpions, bees and wasps. Many venom toxins act as blockers of ions channels and are of use in research because of their potency and high degree of selectivity for their target channel. A number of marketed medicines are based on peptides derived from animal venoms, including the analgesic ziconotide (Prialt), which originates from a cone snail and acts as a calcium channel blocker. Below is an example of an ion channel blocker, available from Tocris, which is the active ingredient of a venom.


By Dick culbert from Gibsons, B.c., canada – Dendroaspis polylepis – the Black Mamba, cc BY 2.0, https://commons.wikimedia.org/w/index.php?curid=50155545

Ion channeLS

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4231 nateglinide Kir6 (KaTP) blocker; displays high affinity for SUR1/Kir6.2 channels 10 mg

50 mg

2095 PnU 37883 Vascular Kir6 (KaTP) channel blocker 10 mg

50 mg

3805 Repaglinide Kir6 (KaTP) channel blocker 50 mg

0925 Sch 23390 Kir3 channel blocker; standard selective D1-like antagonist; also 5-hT2c and 5-hT1c agonist

10 mg

50 mg

4339 Tertiapin LQ Selective Kir1.1 blocker; derivative of tertiapin-Q (cat. no. 1316) 1 mg

1316 Tertiapin-Q Selective blocker of inward-rectifier K+ channels 1 mg

3891 VU 590 Inhibitor of Kir1.1 (RoMK) and Kir7.1 10 mg

50 mg

4197 VU 591 Selective Kir1.1 (RoMK) inhibitor 10 mg

50 mg

two-P Potassium Channels

Activators 3797 BL 1249 Putative K2P2.1 (TReK-1) channel opener 10 mg

50 mg

Blockers 5337 ML 365 Potent and selective TaSK-1 channel blocker 10 mg

50 mg

5338 PK-ThPP Potent TaSK-3 channel blocker 10 mg

50 mg

5594 Spadin Potent TReK-1 channel blocker 1 mg

Voltage-gated Potassium (Kv) Channels

Activators 2867 Flupirtine KV7 channel activator 10 mg

50 mg

4519 ML 213 KV7.2 and KV7.4 channel opener 10 mg

50 mg

3062 nS 1643 KV11.1 (heRG) channel activator; antiarrhythmic 10 mg

50 mg

5083 Qo 58 KV7 channel opener 10 mg

50 mg

Blockers 0940 4-aminopyridine non-selective KV channel blocker 100 mg

5659 ammTX3 KV4 channel blocker 10 μg

3489 astemizole KV11.1 (heRG) channel blocker; also orally active, potent h1 antagonist 50 mg

5929 BeKm 1 Potent and selective KV11.1 (heRG) channel blocker 100 μg

1808 e-4031 KV11.1 (heRG) channel blocker; inhibits rapid delayed rectifier K+ current (IKr)

10 mg

50 mg

5676 Guangxitoxin 1e Potent KV2.1 and KV2.2 channel blocker 100 μg

5011 hMR 1556 Potent and selective IKs channel blocker 10 mg

3899 JnJ 303 Potent and selective IKs blocker 10 mg

50 mg

3564 Kaliotoxin KV and Kca blocker 100 μg

1278 Kn 93 caM kinase II inhibitor; also K+ channel blocker (KV) 1 mg

1999 Linopirdine KV7 (KcnQ) channel blocker 10 mg

50 mg

3563 Margatoxin Potent KV1.3 channel blocker 100 μg

2000 Xe 991 Potent, selective KV7 (KcnQ) channel blocker; blocks M-currents 10 mg

50 mg

Others 2787 BaPTa aM Blocks hKV1.5, hKV11.1 (heRG) and hKV1.3 channels; also cell-permeable ca2+ chelator

25 mg

5858 Droperidol exhibits affinity for heRG channels; also D2 receptor antagonist 50 mg

non-selective / other Potassium Channels

Blockers 4739 cesium chloride Potassium channel blocker; neuroprotective 50 mg

2330 DMP 543 K+ channel blocker and potent ach release enhancer 10 mg

50 mg

Others 0416 YS-035 Inhibits K+ outward/pacemaker current 10 mg

50 mg




20 |

SodiumChannelsVoltage-gated sodium Channels

Activators 5941 oD1 Potent hnav1.4, rnav1.6 and rnav1.7 channel activator 10 μg

2918 Veratridine Voltage-gated na+ channel opener 10 mg

50 mg

Blockers 6159 4,9-anhydrotetrodotoxin Potent and selective nav1.6 channel blocker 100 μg

1470 Flecainide acetate cardiac na+ channel blocker; antiarrhythmic 10 mg

50 mg

4718 huwentoxin IV Selective nav1.7 channel blocker 100 μg

5066 Ica 121431 Potent and selective nav1.3 and nav1.1 channel blocker 10 mg

50 mg

5931 PF 05089771 Potent and selective nav1.7 channel blocker 10 mg

50 mg

5792 ProTx III Potent nav1.7 blocker; analgesic 100 μg

1014 QX 314 bromide na+ channel blocker 100 mg

2313 QX 314 chloride na+ channel blocker 50 mg

0768 Riluzole Blocks voltage-dependent na+ channels; also glutamate release inhibitor/GaBa uptake inhibitor

25 mg

1078 Tetrodotoxin na+ channel blocker 1 mg

1069 Tetrodotoxin citrate na+ channel blocker; citrate salt of tetrodotoxin (cat. no. 1078) 1 mg

2815 Valproic acid, sodium salt Blocks voltage-dependent na+ channels; also histone deacetylase inhibitor

100 mg

TransientReceptorPotentialChannelstRPA1

Activators 5178 aSP 7663 Selective TRPa1 activator 10 mg

50 mg

Blockers 2896 hc 030031 Selective TRPa1 blocker 10 mg

50 mg

tRPC

Activators 4522 Flufenamic acid activates TRPc6; nSaID 50 mg

Blockers 5371 clemizole TRPc5 blocker; also h1 antagonist 10 mg

50 mg

4912 GsMTx4 TRPc1 and TRPc6 blocker; inhibits mechanosensitive ion channels 100 μg

5807 M 084 TRPc4/5 channel blocker; antidepressant and anxiolytic 10 mg

50 mg

4732 ML 204 Selective TRPc4 blocker 10 mg

50 mg

3751 Pyr3 Selective TRPc3 blocker 10 mg

50 mg

tRPM

Activators 5521 cIM 0216 Selective TRPM3 agonist 10 mg

50 mg

1531 Icilin activates a novel cold receptor. cooling agent 10 mg

50 mg

3040 WS 12 TRPM8 agonist; cooling agent 10 mg

50 mg

2927 WS 3 TRPM8 agonist; cooling agent 10 mg

50 mg

Blockers 3989 aMTB TRPM8 blocker 10 mg

50 mg

5324 M8 B Potent and selective TRPM8 channel blocker 10 mg

50 mg

5143 ononetin TRPM3 blocker 50 mg

6003 PF 0515679 Selective TRPM8 blocker 10 mg

4999 9-Phenanthrol Selective TRPM4 blocker 50 mg

5388 RQ 00203078 Potent and selective TRPM8 antagonist; orally active 10 mg

50 mg


Ion channeLS

www.tocris.com | 21

5410 Tc-I 2014 Potent TRPM8 antagonist 10 mg

50 mg

4632 Tc-I 2000 TRPM8 blocker 10 mg

50 mg

tRPML

Activators 5547 MK6-83 TRPML channel activator 10 mg

50 mg

4746 ML Sa1 activator of TRPML channels 10 mg

50 mg

4907 Sn 2 Selective TRPML3 channel activator 10 mg

50 mg

tRPP

Blockers 3378 eIPa Inhibits TRPP3-mediated currents; also inhibits the na+/h+ exchanger (nhe)

10 mg

50 mg

3379 Phenamil Inhibits TRPP3-mediated currents; also inhibits epithelial na+ channels

10 mg

50 mg

tRPV

Agonists 1116 aM 404 Vanilloid receptor agonist; also anandamide transport inhibitor 10 mg

50 mg

1339 anandamide endogenous TRPV1 and cB receptor agonist 5 mg

25 mg

1017 anandamide (in Tocrisolve™ 100) endogenous TRPV1 and cB receptor agonist (in water-soluble emulsion)

10 mg

50 mg

1354 arvanil Potent TRPV1 and cB1 agonist; also anandamide transport inhibitor 5 mg

25 mg

Stem Cell feature products

NH

OMe

O

MeMe

O2N

F3C

(±)-Bay K 8644 (1544)Potent L-type (voltage-gated)

Ca2+ channel blocker

FN

O OMe

Me

O

N

HN

Mibefradil (2198)T and L-type (voltage-gated) Ca2+

channel blocker

NO2

NH

CO2Me

MeMe

MeO2C

Nifedipine (1075) L-type (voltage-gated) Ca2+

channel blocker

N O

NN

Linopirdine (1999)Voltage-gated potassium channel blocker;

blocks KV 7.1 + 7.3 (M-currents) and KV 7.1 (KCNQ1) homomeric channels

O

N N

XE 991 (2000)Potent and selective voltage-gated potassium

channel blocker. Blocks K V 7.2+7.3 (M-currents) and KV 7.1 homomeric channels

Cl

Cl

S S

NN

N

N

Yoda 1 (5586)Piezo1 channel activator

Ion Channels in Stem Cell Research:A variety of ion channels are expressed by stem cells and have recently been shown to have a role in the regulation of self-renewal, differentiation and maturation of cells. Blockade or activation of ion channels may impact on the differentiation of stem cells towards certain lineages. Pharmacological reagents targeting ion channels can also be used to characterize differentiated cells. Research in this area is of interest in tissue repair, for example wound healing or neurodegenerative diseases, disease modeling, drug target discovery and toxicity testing. Below is a selection of compounds that may be of use in determining how specific channels function to direct the differentiation of stem cells.




22 |

0462 (e)-capsaicin Prototypic vanilloid receptor agonist 100 mg

1556 6ʹ-Iodoresiniferatoxin high affinity TRPV1 agonist/partial agonist 1 mg

1568 naDa Vanilloid agonist; also endogenous cB1 agonist and inhibitor of Faah and aMT

5 mg

25 mg

1641 oLDa Potent, selective endogenous TRPV1 agonist 5 mg

25 mg

0934 olvanil Potent vanilloid receptor agonist 10 mg

50 mg

1466 PPahV non-pungent vanilloid receptor agonist 1 mg

1137 Resiniferatoxin Potent vanilloid receptor agonist 1 mg

3745 Rn 1747 Selective TRPV4 agonist 10 mg

50 mg

Antagonists 5781 a 425619 Potent TRPV1 antagonist 10 mg

50 mg

4319 a 784168 Potent and selective TRPV1 antagonist 10 mg

50 mg

4330 aMG 21629 Potent and selective TRPV1 antagonist 1 mg

5995 aMG 517 Potent TRPV1 antagonist 10 mg

50 mg

2316 aMG 9810 Potent and selective, competitive antagonist of TRPV1 10 mg

50 mg

2836 arachidonyl serotonin Dual TRPV1 antagonist/Faah inhibitor 10 mg

3875 BcTc TRPV1 antagonist 10 mg

50 mg

5106 GSK 2193874 Potent and selective TRPV4 antagonist; orally active 10 mg

50 mg

4100 hc 067047 Potent and selective TRPV4 antagonist 10 mg

50 mg

1975 6-Iodonordihydrocapsaicin Potent, competitive vanilloid receptor antagonist 10 mg

50 mg

3361 JnJ 17203212 Reversible, competitive and potent TRPV1 antagonist 10 mg

50 mg

1577 L-R4W2 TRPV1 antagonist peptide 1 mg

3746 Rn 1734 Selective TRPV4 antagonist 10 mg

50 mg

5678 Rn 9893 Potent and selective TRPV4 antagonist 10 mg

50 mg

1615 SB 366791 Potent, selective, competitive TRPV1 antagonist 10 mg

50 mg

3265 SB 452533 Potent TRPV1 receptor antagonist 10 mg

50 mg

4729 α-Spinasterol TRPV1 antagonist; active in vivo 1 mg

Others 5246 MRS 1477 TRPV1 positive allosteric modulator 10 mg

50 mg

2203 PaLDa endogenous lipid; potentiates effects of endovanilloids at TRPV1 receptors

10 mg

2204 STeaRDa endogenous lipid, active in vivo; enhances effects of endovanilloids at TRPV1 receptors

10 mg

1098 Tranilast Inhibits TRPV2-mediated responses; also inhibits inflammatory mediator release from mast cells

10 mg

50 mg


Ion channeLS

www.tocris.com | 23

The Comprehensive in Vitro Proarrhythmia Assay (CiPA) Initiative:Prior to 2005, a number of medicines were withdrawn from the market following the finding that they delayed ventricular repolarization (prolongation of the QTc interval in the ECG) causing serious arrhythmias, known as Torsades de Pointes (TdP). This life-threatening effect was found to result from the ability of these drugs to block voltage-gated potassium channels (Kv11.1 or hERG). Among drugs withdrawn from the market owing to proarrhythmic effects were: the antihistamine astemizole, the antibiotic grepafloxacin, and the treatment for gastroesophageal reflux, cisapride.

In 2005 new regulatory guidelines, E14 and ICH S7B, were introduced requiring all new drugs to be tested for their effects on the QT interval in both clinical and preclinical tests. These guidelines have proved effective in preventing the introduction of new medicines that might cause TdP. However, Kv11.1 is only one of several ion channels controlling ventricular repolarization, but E14 and ICHS7B focus only on the effect of compounds on Kv11.1 channels, so there is a possibility that these guidelines may prevent the further development of useful drugs that induce QTc prolongation, but do not increase the risk of TdP.

The Comprehensive in Vitro Proarrhythmia Assay (CiPA) initiative has been established to address this situation and aims to develop a new mechanism for assessing the proarrhythmia risk of drugs in development, with a view to revising current guidelines for approval of medicines. CiPA will have four main components: in vitro ion channel assays; computer modeling of cardiac electrophysiology; confirmation of activity in stem cell-derived cardiomyocytes; and clinical assessment of electrophysiologic effects in phase I ECG studies. For the in vitro assays, voltage clamp protocols have been developed for key cardiac ion channels, including Kv11.1, Nav1.5, Cav1.2, Kv4.3, Kir2.1, KCNQ + KCNE, to test new drugs.

In addition the CiPA steering group has generated a list of 28 drugs with known effects on cardiac electrophysiology, categorized as having high, intermediate or low risk of TdP. These drugs can be used for assay validation and calibration.

CiPA Compound Test Set

High Risk Intermediate Risk Low risk

azilimide astemizole Diltiazem

Bepridil chlorpromazine Loratadine

Dofetilide cisapride Metoprolol

Ibutilide clarithromycin Mexiletine

Quinidine clozapine nifedipine

Vandetanib Domperidone nitrendipine

Disopyramide Droperidol Ranolazine

D,L-Sotalol Terfenadine Tamoxifen

Pimozide Verapamil

Risperidone

ondansetron

QT interval

PQ S

T

R

Normal ECG Trace


24 |

AquaporinsBlockers 5412 Tc aQP1 1 aquaporin 1 (aQP1) channel blocker 10 mg

50 mg

5425 TGn 020 aquaporin 4 (aQP4) channel blocker 10 mg

50 mg

ChlorideChannelsCalcium-activated Chloride Channels

Activators 4876 eact activator of ca2+-activated cl– channel transmembrane protein 16a (TMeM16a)

10 mg

50 mg

Blockers 6076 ani 9 Potent and selective TMeM16a (anoctamin-1; ano1) blocker 10 mg

50 mg

5420 Benzbromarone TMeM16a/B calcium-activated chloride channel (cacc) blocker 50 mg

4877 caccinh-a01 calcium-activated chloride channel (cacc) inhibitor 10 mg

50 mg

5770 Monna Potent TMeM16a (anoctamin-1) blocker 10 mg

50 mg

0593 nPPB Inhibits calcium-sensitive chloride currents 50 mg

4538 T16ainh - a01 ca2+-activated cl– channel transmembrane protein 16a (TMeM16a) inhibitor

10 mg

50 mg

2510 Talniflumate cacc blocker and cl–/hco3– exchange inhibitor 10 mg

50 mg

CFtR

Activators 1422 DceBIo activates cl- conductance and hKca3.1 channels 10 mg

50 mg

Blockers 3430 cFTRinh 172 Voltage-independent, selective cFTR chloride channel blocker 10 mg

50 mg

5485 Glyh 101 Reversible, voltage-dependent cFTR chloride channel blocker 10 mg

50 mg

1646 Lonidamine cFTR cl- channel blocker; also mitochondrial hexokinase inhibitor 10 mg

50 mg

4303 PPQ 102 Potent, voltage-independent cFTR chloride channel inhibitor 10 mg

50 mg

Others 3143 KM 11060 corrects F508del-cFTR trafficking 10 mg

50 mg

3943 PG 01 cFTR mutants potentiator 10 mg

50 mg

other Chloride Channels

Blockers 1540 DcPIB Selective blocker of VSac/Icl, swell; inhibits glucose-stimulated insulin release

10 mg

50 mg

4523 DIDS cIc-Ka chloride channel blocker; TRPV1 modulator; RaD51 recombinase inhibitor

50 mg

4911 GaTx2 high affinity, selective clc-2 blocker; inhibits slow-gating 100 μg

Others 0963 9-ac chloride transport inhibitor; also inhibits PKa activated cardiac Icl 100 mg

IonophoresOthers 1234 a23187, free acid calcium ionophore 10 mg

1704 Ionomycin calcium salt calcium ionophore 1 mg

2092 Ionomycin free acid calcium ionophore 1 mg

5223 Monensin sodium salt Sodium ionophore; antibacterial agent 500 mg

4312 nigericin sodium salt Selective K+ ionophore 10 mg

2505 nonactin Monovalent cation ionophore 10 mg

3373 Valinomycin Selective K+ ionophore 10 mg

50 mg

other channelsThis group includes compounds targeting chloride channels, aquaporins (channels that allow the passage of water), ionophores (ion carrying compounds), photoswitchable ligands and compounds that modulate multiple ion channels.


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www.tocris.com | 25

PhotoswitchableLigandsOthers 5462 aaQ chloride Photoswitchable Kv channel blocker 10 mg

50 mg

5464 ac 4 Photoswitchable TRPV1 channel blocker 10 mg

50 mg

5463 Pa 1 Photoswitchable enac blocker 10 mg

50 mg

5470 QaQ dichloride Photoswitchable nav, Kv and cav channel blocker 10 mg

50 mg

OtherChannelModulatorsOthers 4095 amiodarone Broad spectrum ion channel blocker; antiarrhythmic 50 mg

2090 caLP1 cell-permeable calmodulin agonist 1 mg

5449 erastin Mitochondria VDac modulator; also Ferroptosis activator 10 mg

3908 Ibutilide Blocks IKr, heRG and L-type ca2+ channels; class III antiarrhythmic 50 mg

1611 Lamotrigine Blocks na+, K+ and ca2+ channels; also inhibits glutamate release. anticonvulsant

10 mg

50 mg

2289 Lamotrigine isethionate Inhibits glutamate release. Water-soluble salt of lamotrigine (cat. no. 1611)

10 mg

50 mg

2314 Loe 908 Broad spectrum cation channel blocker; neuroprotective 10 mg

50 mg

2851 nefiracetam activates L/n-type calcium channels, cholinergic, monoaminergic vand GaBaergic systems; cognitive enhancer

100 mg

3692 4,4-Pentamethylenepiperidine M2 proton channel blocker 50 mg

4108 Quinidine Blocks sodium and potassium channels 50 mg

2906 TRo 19622 Binds voltage-dependent anion channel (VDac) 10 mg

50 mg

2625 Zonisamide Blocks voltage-sensitive na+ and ca2+ channels (T-type) 10 mg

50 mg


Scientific ReviewsProduct Guides & Listings Life Science Posters

• neurodegeneration • Pain Research• cardiovascular Research

• Learning and Memory • antidepressants • Multiple Sclerosis • Peripheral Sensitization

• nicotinic ach Receptors• neuronal 5hT Receptors• GaBa Receptors• P2X and P2Y Receptors

Other Life Science Literature from TocrisTocris also provides a wide range of scientific literature free of charge, including the following titles:

To download or request copies, please visit www.tocris.com/requestliterature


26 |

a Selection of antibodies Targeting Ion channels available from Bio-Techne

Species Molecule Description Antibody ApplicationsLigand-gated Ion Channels

epithelial sodium Channels

aF2968 Mouse Prostasin/Prss8 Mouse Prostasin/Prss8 affinity Purified Polyclonal ab eLISa capture (Matched antibody Pair), WB

aF4599 human Prostasin/Prss8 human Prostasin/Prss8 affinity Purified Polyclonal ab Ihc, IP, Simple Western, WB

MaB4599 human Prostasin/Prss8 human Prostasin/Prss8 Mab (clone 530622) Ihc, IP, WB

GABA-A Receptors

aF1188 Rat GaBa-B R2 Rat GaBa-B-R2 affinity Purified Polyclonal ab Ihc, WB

aF5590 human GaBa-a R beta 3 human GaBa-a-R beta 3 affinity Purified Polyclonal ab Ihc, Simple Western, WB

aF7000 human/Mouse/Rat GaBa-B R1 human/Mouse/Rat GaBa-B-R1 affinity Purified Polyclonal ab Ihc, WB

MaB7000 Rat GaBa-B R1 Rat GaBa-B-R1 Mab (clone 751216) Ihc

PPS022 human/Mouse/Rat/Bovine/canine/Primate/Zebrafish

GaBa-a R alpha 1 GaBa-a-R alpha 1 c-Terminus affinity Purified Polyclonal ab WB

PPS023 Mouse/Rat/Bovine GaBa-a R alpha 1 Mouse/Rat GaBa-a-R alpha 1 n-Terminus affinity Purified Pab WB

PPS024 human/Mouse/Rat/Bovine/canine/Primate

GaBa-a R alpha 2 human/Mouse/Rat/Bovine GaBa-a-R alpha 2 Polyclonal ab WB

PPS025 human/Mouse/Rat/Bovine/canine/Primate/Zebrafish

GaBa-a R alpha 4 GaBa-a-R alpha 4 c-Terminus affinity Purified Polyclonal ab WB

PPS027 Mouse/Rat GaBa-a R alpha 5 Mouse/Rat GaBa-a-R alpha 5 c-Terminus affinity Purified Pab WB

PPS030 human/Mouse/Rat GaBa-a R beta 1 GaBa-a-R beta 1 c-Terminus affinity Purified Polyclonal ab WB

PPS031 human/Mouse/Rat/Bovine/canine/Primate

GaBa-a R beta 2 GaBa-a-R beta 2 c-Terminus affinity Purified Polyclonal ab WB

PPS072 human/Mouse/Rat/Bovine/chicken/Primate/Zebrafish

GaBa-a R gamma 2 human/Mouse/Rat/Bovine GaBa-a-R gamma 2 Polyclonal ab WB

PPS073 human/Mouse/Rat/Xenopus GaBa-B R2 Phospho-GaBa-B-R2 (S892) affinity Purified Polyclonal ab IF, WB

PPS090 human/Mouse/Rat/Bovine GaBa-a R delta GaBa-a-R delta n-Terminus affinity Purified Pab Ihc, IP, WB

Ionotropic Glutamate Receptors

aF4514 human mGluR5 human mGluR5 affinity Purified Polyclonal ab Ihc, WB

aF4668 human mGluR3 human mGluR3 affinity Purified Polyclonal ab Ihc, WB

aF4836 human mGluR1 human mGluR1 affinity Purified Polyclonal ab WB

aF7387 human mGluR4 human mGluR4 affinity Purified Pab cyToF-ready, Flow cytometry, Ihc

aF8138 human hcn4 human hcn4 affinity Purified Polyclonal ab Icc

MaB4405 human mGluR7 human mGluR7 Mab (clone 437310) cyToF-ready, Flow cytometry

MaB4514 human mGluR5 human mGluR5 Mab (clone 464818) cyToF-ready, Intracellular Staining by Flow cytometry, WB

MaB45141 human mGluR5 human mGluR5 Mab (clone 464823) Ihc

MaB4676 human mGluR2 human mGluR2 Mab (clone 455310) cyToF-ready, Intracellular Staining by Flow cytometry, WB

MaB4836 human mGluR1 human mGluR1 Mab (clone 511622) Ihc

MaB5277 human mGluR8 human mGluR8 Mab (clone 476410) Ihc, WB

MaB8138 human hcn4 human hcn4 Mab (clone 880904) Icc

PPS007 human/Mouse/Rat/canine/chicken

GluR1 Phospho-GluR1 (S831) affinity Purified Polyclonal ab WB

PPS008 human/Mouse/Rat/Primate GluR1 Phospho-GluR1 (S845) affinity Purified Polyclonal ab WB

PPS009 Rat Glycine R Rat Glycine R affinity Purified Polyclonal ab Ihc, WB

PPS011B human/Mouse/Rat GRIn1/nMDaR1 human/Mouse/Rat GRIn1/nMDaR1 Mab (clone R1JhL) IP, WB

PPS033 human/Mouse/Rat GRIn2c/nMDaR2c human/Mouse/Rat GRIn2c/nMDaR2c affinity Purified Pab IP, WB

PPS051 human/Mouse/Rat/chicken/Zebrafish

GluR2/3 human/Mouse/Rat GluR2/3 affinity Purified Polyclonal ab WB

PPS080 Mouse/Rat GRIn1/nMDaR1 Mouse/Rat GRIn1/nMDaR1 Variant c1 affinity Purified Pab Ihc, WB

PPS081 Mouse/Rat GRIn1/nMDaR1 Mouse/Rat GRIn1/nMDaR1 Variant c2 affinity Purified Pab Ihc, WB

PPS082 human/Mouse/Rat GRIn1/nMDaR1 GRIn1/nMDaR1 Variant c2’ affinity Purified Polyclonal ab Ihc, WB

PPS083 Mouse/Rat GRIn1/nMDaR1 Mouse/Rat GRIn1/nMDaR1 Variant n1 affinity Purified Pab Ihc, WB

Voltage-gated Ion Channels

Potassium Channels

aF2360 human DPP6 human DPP6 affinity Purified Polyclonal ab cyToF-ready, Flow cytometry, Ihc, IP, WB

MaB2360 human DPP6 human DPP6 Mab (clone 274308) cyToF-ready, Flow cytometry, IP

MaB23601 human DPP6 human DPP6 ectodomain Mab (clone 274311) IP, WB

MaB4100 human DPP10 human DPP10 Mab (clone 453601) WB

PPS015 Rat/Xenopus Potassium channel Kv2.2

Potassium channel Kv2.2 affinity Purified Pab Ihc, WB

PPS016 Mouse/Rat Potassium channel Kv3.1

Phospho-Potassium channel Kv3.1 (S503) affinity Purified Pab Ihc, WB

other Channels

CFtR

MaB1660 human cFTR human cFTR R Domain Mab (clone 13-1) IF, Ihc, IP, WB

MaB25031 human cFTR human cFTR c-Terminus Mab (clone 24-1) Ihc, IP, WB

Icc, immunocytochemistry; IF, immunofluorescence; Ihc, immunohistochemistry; IP, immunoprecipitation; WB, Western Blot.

Find out more at bio-techne.com

Ion channeLS

www.tocris.com | 27

References

Category Authors Year Title Journal Vol Page

Pharmacology clapham et al. 2003 International Union of Pharmacology. XLIII. compendium of voltage-gated ion channels: transient receptor potential channels.

Pharmacol.Rev. 55 591

Goldstein et al. 2005 International Union of Pharmacology. LV. nomenclature and molecular relationships of two-P potassium channels.


Gutman et al. 2005 International Union of Pharmacology. LIII. nomenclature and molecular relationships of voltage-gated potassium channels.


Verkman and Galietta

2009 chloride channels as drug targets. Nat.Rev.Drug.Discov. 8 153

Kellenberger and Schild

2014 International Union of Basic and clinical Pharmacology Review. XcI. Structure, function, and pharmacology of acid-sensing channels (aSIcs) and the epithelial na+ channel.

67 1

Boscardin et al. 2016 International Union of Basic and clinical Pharmacology Review. The function and regulation of acid-sensing channels (aSIcs) and the epithelial na+ channel (enac): IUPhaR review 19.

Br.J.Pharmacol. 173 2671

Ion Channels in Cancer Research

Djamgoz et al. 2014 Theme Issue. Ion transport and cancer: from initiation to metastasis.

Philos.Trans.R.Soc.B. Biol.Sci.

369

Ion Channels in Immunology Research

Feske et al. 2012 Ion channels and transporters in lymphocyte function and immunity.

Nat.Rev.Immunol. 12 532

Feske et al. 2015 Ion channels in innate and adaptive immunity. Annu.Rev.Immunol. 33 291

Vig and Kinet 2009 calcium signaling in immune cells. Nat.Immunol. 10 21

Stebbing et al. 2015 The role of ion channels in microglial activation and proliferation – a complex interplay between ligand-gated ion channels, K+ channels, and intracellular ca2+.

Front.Immunol. 6 497

Ion Channels in Stem Cell Research

Pathak et al. 2014 Stretch-activated ion channel Piezo1 directs lineage choice in human neural stem cells.

Proc.Natl.Acad.Sci.U.S.A. 111 16148

nguemo et al. 2013 The L-type ca2+ channel blocker nifedipine represses mesodermal fate determination in murine embryonic stem cells.

PLoS One 8 e53407

Iannotti et al. 2009 expression, localization, and pharmacological role of KV7 potassium channels in skeletal muscle proliferation, differentiation, and survival after myotoxic insults.

J.Pharmacol.Exp.Ther. 332 811

Zhou et al. 2011 Potential role of KcnQ/M-channels in regulating neuronal differentiation in mouse hippocampal and embryonic stem cell-derived neuronal cultures.

Exp.Neurol. 229 471

Rodríguez-Gómez et al.

2012 T-type ca2+ channels in mouse embryonic stem cells: modulation during cell cycle and contribution to self-renewal.

Am.J.Physiol.Cell Physiol. 302 c494

Ge et al. 2013 Distal c terminus of caV1.2 channels plays a crucial role in the neural differentiation of dental pulp stem cells.

PLoS One 8 e81332

CiPA colatsky et al. 2016 The comprehensive in vitro proarrhythmia assay (ciPa) initiative – update on progress.

J.Pharmacol.Toxicol.Methods

81 233

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Ion Channels - Tocris Bioscience · 2017-06-19 · Ion channels are pore-forming proteins present in the plasma membrane of most cells, as well as the intracellular membranes surrounding