Potassium Channel

Inhibitory Selectivity

Potassium Channel Products

New Potassium Channel Products
Catalog No. Information Product Use Citations Product Validations
S2825

ML133 HCl

ML133 HCl is a selective potassium channel inhibitor for Kir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on Kir1.1 and weak activity for Kir4.1 and Kir7.1.

S4489New

Tetraethylammonium chloride

Tetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties.

S4495New

Quinine

Quinine, an alkaloid derived from the bark of the cinchona tree, is an anti-malaria agent and a potassium channel inhibitor that inhibits mSlo3 (KCa 5.1) channel currents evoked by voltage pulses to +100 mV with IC50 of 169 μM.

S4681New

Quinidine hydrochloride monohydrate

Quinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM.

S9223

Talatisamine

Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.

E0001New

DCPIB

DCPIB is a specific and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB potently inhibits several K2P channels with no voltage dependence, including TRESK, TASK1, and TASK3. DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels. DCPIB is also a novel selective blocker of I(Cl,swell), which blocks native I(Cl,swell) of calf bovine pulmonary artery endothelial (CPAE) cells with an IC(50) of 4.1 μM.

E0012New

1-EBIO

1-EBIO (1-Ethylbenzimidazolinone, 1-Ethyl-2-benzimidazolinone)is an activator of Ca2+-sensitive K+ channels with an EC50 of 490 µM in T84 cells.

S4439New

Almitrine mesylate

Almitrine mesylate (Almitrine bismesylate, Almitrine dimethanesulfonate, Almitrine dimesylate), a pharmacologically unique respiratory stimulant, acts as an agonist of peripheral chemoreceptors located on the carotid bodies. Almitrine mesylate inhibits the activity of Ca2+-dependent K+ channel by decreasing its open probability with IC50 of 0.22 μM.

S2967New

XE991 dihydrochloride

XE 991 (LS190926) dihydrochloride is a blocker of Kv7 (KCNQ) channels that potently inhibits KCNQ1 (Kv7.1), KCNQ2 (Kv7.2), KCNQ2 + KCNQ3 (Kv7.3) channel, and M-current with IC50 of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively.

S0524

A2793

A2793 (Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate) is an efficient inhibitor of TWIK-related spinal cord potassium channel (TRESK, K2P18, KCNK18) and TASK-1 (KCNK3) with IC50 of 6.8 μM for mouse TRESK.

S3242

Loureirin B

Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular.

S0741

A2764 dihydrochloride

A2764 dihydrochloride is a selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1) with IC50 of 11.8 μM for the activated mTRESK channel. A2764 dihydrochloride has the potential for probing the role of TRESK channel in migraine and nociception.

S9251

Oxypeucedanin

Oxypeucedanin is a major coumarin aglycone that can be extracted from Ostericum koreanum. It is a kind of open-channel blocker of the hKv1.5 channel.

S0087

JNJ 303

JNJ 303 is a potent blocker of the voltage dependent IKs-channel encoded by KCNQ1/KCNE1 with IC50 of 64 nM. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP).

S6554

ML365

ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3).

S2405

Sophocarpine

Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.

S0398

Astemizole

Astemizole (R 43512) is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects.

S0188

GSK369796 Dihydrochloride

GSK369796 Dihydrochloride (N-tert-butylisoquine) is an inhibitor of hERG potassium ion channel repolarization with IC50 of 7.5 μM. GSK369796 Dihydrochloride is an affordable and effective 4-aminoquinoline antimalarial.

S5773

NS1643

NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents.

S0476

SCH-23390 hydrochloride

SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.

S6627

E-4031 dihydrochloride

E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type.

E0030New

NS309

NS309 is a potent and selective activator of human Ca2+ -activated K+ channels of SK and IK types with an EC50 of 150  nM for hSK3 channel, and displays no activity at BK channels.

S6559

ML-297

ML-297 (VU 0456810, CID 56642816) is a potent and selective activator of Kir3.1/3.2 (G protein-coupled inwardly rectifying potassium, GIRK1/2) channel with EC50 of 0.16 μM and 1.8 μM for GIRK1/2 and GIRK1/4, respectively. ML-297 is potential for the treatment of epilepsy.

S6553

ML213

ML213 (CID-3111211) is a selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) potassium channel opener with EC50 of 230 nM and 510 nM, respectively.

S0144

ICA 069673

ICA 069673 (compound 51) is an orally active, potent and selective KCNQ2/Q3 potassium channel activator with EC50 of 0.69 μM and 14.3 μM for KCNQ2/Q3 and KCNQ3/Q5, respectively.

S6572

ML335

ML335 is a potent and selective TREK-1/2 activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.

S0462

NS-1619

NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels.

S0467

Emodepside

Emodepside (QHT06, BAY 44-4400, PF 1022-221), a semisynthetic derivative of PF1022A, is a cyclooctadepsipeptide with broad-spectrum anthelmintic activity. Emodepside activates Ca-dependent SLO-1-like K channels.

S0075

ICA-110381

ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 exhibits KCNQ2/Q3 agonist activity with EC50 of 0.38 μM and KCNQ1 antagonist activity with IC50 of 15 μM, respectively.

S6653

Nigericin (NSC 292567) sodium salt

Nigericin (NSC 292567) sodium salt is an antibiotic derived from Streptomyces hygroscopicus that works by acting as an H+, K+, and Pb2+ ionophore.Nigericin can activate NLRP3 inflammasome to induce pro-inflammatory and immunostimulatory processes.

Catalog No. Information Product Use Citations Product Validations
S2825

ML133 HCl

ML133 HCl is a selective potassium channel inhibitor for Kir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on Kir1.1 and weak activity for Kir4.1 and Kir7.1.

S4489New

Tetraethylammonium chloride

Tetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties.

S4495New

Quinine

Quinine, an alkaloid derived from the bark of the cinchona tree, is an anti-malaria agent and a potassium channel inhibitor that inhibits mSlo3 (KCa 5.1) channel currents evoked by voltage pulses to +100 mV with IC50 of 169 μM.

S4681New

Quinidine hydrochloride monohydrate

Quinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM.

S9223

Talatisamine

Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.

E0001New

DCPIB

DCPIB is a specific and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB potently inhibits several K2P channels with no voltage dependence, including TRESK, TASK1, and TASK3. DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels. DCPIB is also a novel selective blocker of I(Cl,swell), which blocks native I(Cl,swell) of calf bovine pulmonary artery endothelial (CPAE) cells with an IC(50) of 4.1 μM.

E0012New

1-EBIO

1-EBIO (1-Ethylbenzimidazolinone, 1-Ethyl-2-benzimidazolinone)is an activator of Ca2+-sensitive K+ channels with an EC50 of 490 µM in T84 cells.

S4439New

Almitrine mesylate

Almitrine mesylate (Almitrine bismesylate, Almitrine dimethanesulfonate, Almitrine dimesylate), a pharmacologically unique respiratory stimulant, acts as an agonist of peripheral chemoreceptors located on the carotid bodies. Almitrine mesylate inhibits the activity of Ca2+-dependent K+ channel by decreasing its open probability with IC50 of 0.22 μM.

S2967New

XE991 dihydrochloride

XE 991 (LS190926) dihydrochloride is a blocker of Kv7 (KCNQ) channels that potently inhibits KCNQ1 (Kv7.1), KCNQ2 (Kv7.2), KCNQ2 + KCNQ3 (Kv7.3) channel, and M-current with IC50 of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively.

S0524

A2793

A2793 (Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate) is an efficient inhibitor of TWIK-related spinal cord potassium channel (TRESK, K2P18, KCNK18) and TASK-1 (KCNK3) with IC50 of 6.8 μM for mouse TRESK.

S3242

Loureirin B

Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular.

S0741

A2764 dihydrochloride

A2764 dihydrochloride is a selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1) with IC50 of 11.8 μM for the activated mTRESK channel. A2764 dihydrochloride has the potential for probing the role of TRESK channel in migraine and nociception.

S9251

Oxypeucedanin

Oxypeucedanin is a major coumarin aglycone that can be extracted from Ostericum koreanum. It is a kind of open-channel blocker of the hKv1.5 channel.

S0087

JNJ 303

JNJ 303 is a potent blocker of the voltage dependent IKs-channel encoded by KCNQ1/KCNE1 with IC50 of 64 nM. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP).

S6554

ML365

ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3).

S2405

Sophocarpine

Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.

S0398

Astemizole

Astemizole (R 43512) is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects.

S0188

GSK369796 Dihydrochloride

GSK369796 Dihydrochloride (N-tert-butylisoquine) is an inhibitor of hERG potassium ion channel repolarization with IC50 of 7.5 μM. GSK369796 Dihydrochloride is an affordable and effective 4-aminoquinoline antimalarial.

S5773

NS1643

NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents.

S0476

SCH-23390 hydrochloride

SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.

S6627

E-4031 dihydrochloride

E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type.

Catalog No. Information Product Use Citations Product Validations
E0030New

NS309

NS309 is a potent and selective activator of human Ca2+ -activated K+ channels of SK and IK types with an EC50 of 150  nM for hSK3 channel, and displays no activity at BK channels.

S6559

ML-297

ML-297 (VU 0456810, CID 56642816) is a potent and selective activator of Kir3.1/3.2 (G protein-coupled inwardly rectifying potassium, GIRK1/2) channel with EC50 of 0.16 μM and 1.8 μM for GIRK1/2 and GIRK1/4, respectively. ML-297 is potential for the treatment of epilepsy.

S6553

ML213

ML213 (CID-3111211) is a selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) potassium channel opener with EC50 of 230 nM and 510 nM, respectively.

S0144

ICA 069673

ICA 069673 (compound 51) is an orally active, potent and selective KCNQ2/Q3 potassium channel activator with EC50 of 0.69 μM and 14.3 μM for KCNQ2/Q3 and KCNQ3/Q5, respectively.

S6572

ML335

ML335 is a potent and selective TREK-1/2 activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.

S0462

NS-1619

NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels.

S0467

Emodepside

Emodepside (QHT06, BAY 44-4400, PF 1022-221), a semisynthetic derivative of PF1022A, is a cyclooctadepsipeptide with broad-spectrum anthelmintic activity. Emodepside activates Ca-dependent SLO-1-like K channels.

Catalog No. Information Product Use Citations Product Validations
S0075

ICA-110381

ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 exhibits KCNQ2/Q3 agonist activity with EC50 of 0.38 μM and KCNQ1 antagonist activity with IC50 of 15 μM, respectively.

Catalog No. Information Product Use Citations Product Validations
S6653

Nigericin (NSC 292567) sodium salt

Nigericin (NSC 292567) sodium salt is an antibiotic derived from Streptomyces hygroscopicus that works by acting as an H+, K+, and Pb2+ ionophore.Nigericin can activate NLRP3 inflammasome to induce pro-inflammatory and immunostimulatory processes.