Potassium Channel

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Potassium Channel Products

Catalog No. Information Product Use Citations Product Validations
S1658

Dofetilide

Dofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.

S2456

Chlorpromazine HCl

Chlorpromazine HCl (Sonazine) is a dopamine and potassium channel inhibitor with IC50 of 6.1 and 16 μM for inward-rectifying K+ currents and time-independent outward currents.

S1979

Amiodarone HCl

Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.

S1344

Glimepiride

Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.

S1160

TRAM-34

TRAM-34 (Triarylmethane-34) is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450.

S3242New

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.

S0188New

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.

S4353New

Terfenadine

Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

S6627New

E-4031 dihydrochloride

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

S1426

Repaglinide

Repaglinide (AG-EE 623 ZW) is a potassium channel blocker, which lowers blood glucose by stimulating the release of insulin from the pancreas, used the treatment of type II diabetes.

S2502

Quinine HCl Dihydrate

Quinine HCl Dihydrate is a white crystalline K+ channel blocker, used to treat malaria.

S1716

Glyburide (Glibenclamide)

Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.

S2443

Tolbutamide

Tolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes.

S2114

Dronedarone HCl

Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).

S2489

Nateglinide

Nateglinide (A-4166) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.

S8016

Vonoprazan Fumarate (TAK-438)

Vonoprazan Fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion. Phase 3.

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.

S2601

Gliclazide

Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.

S1715

Glipizide

Glipizide (CP-28720) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.

S6284

Tetraethylammonium bromide

Tetraethylammonium bromide is used as the source of tetraethylammonium ions in pharmacological and physiological studies, but is also used in organic chemical synthesis. It blocks selective potassium channels.

S9223

Talatisamine

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

S5371

Ajmaline

Ajmaline, found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent.

S5257

Doxapram

Doxapram is a central respiratory stimulant with a brief duration of action. Doxapram is a selective TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel inhibitor with EC50 of 410 nM, 37 μM, 9 μM, respectively.

S4037

Doxapram HCl

Doxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.

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.

S4583

Butamben

Butamben is a long-duration local anesthetic used for the treatment of chronic pain.

S6554

ML365

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

S4186

Domiphen Bromide

Domiphen bromide (NSC-39415) is a quaternary ammonium antiseptic with actions as a cationic surfactant.

S2405

Sophocarpine

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

S5028

4-Aminopyridine

4-Aminopyridine (4-AP) is a potent and non-selective inhibitor of voltage gated potassium channels (Kv) with IC50 values of 170 μM and 230 μM for Kv1.1 and Kv1.2 in CHO cells, respectively.

S8615

Sodium dichloroacetate (DCA)

Dichloroacetate, a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na+-K+-2Cl- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth.

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.

S2073

Mitiglinide Calcium

Mitiglinide Calcium is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.

S5749

Chlorpromazine

Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.

S6559New

ML-297

ML-297 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.

S0462New

NS-1619

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

S1971

Nicorandil

Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).

S1383

Minoxidil

Minoxidil (U-10858) is a vasodilator medication known for its ability to slow or stop hair loss and promote hair regrowth. Minoxidil is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth.

S2562

Hydralazine HCl

Hydralazine HCl is a hydrochloride salt of hydralazine, which is a direct-acting smooth muscle relaxant used to treat hypertension by acting as a vasodilator primarily in arteries and arterioles.

S4630

Diazoxide

Diazoxide is a well-known small molecule that activates KATP channels in the smooth muscle of blood vessels and pancreatic beta-cells by increasing membrane permeability to potassium ions.

S4733

Retigabine

Retigabine (D-23129) is a novel anticonvulsant with activity in a broad range of seizure models. The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.

S4632

Hexachlorophene

Hexachlorophene (Hexachlorofen, Fostril, Nabac, pHisoHex) is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ± 1.29 μM; It can also attenuate Wnt/beta-catenin signaling through the Siah-1-mediated beta-catenin degradation.

S4734

Retigabine 2HCl

Retigabine is a novel anticonvulsant with activity in a broad range of seizure models. The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.

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.

S0476New

SCH-23390 hydrochloride

SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride,SCH-23390 HCl) 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.

S0398New

Astemizole

Astemizole 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.

S3151

Gliquidone

Gliquidone is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM.

Catalog No. Information Product Use Citations Product Validations
S1658

Dofetilide

Dofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.

S2456

Chlorpromazine HCl

Chlorpromazine HCl (Sonazine) is a dopamine and potassium channel inhibitor with IC50 of 6.1 and 16 μM for inward-rectifying K+ currents and time-independent outward currents.

S1979

Amiodarone HCl

Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.

S1344

Glimepiride

Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.

S1160

TRAM-34

TRAM-34 (Triarylmethane-34) is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450.

S3242New

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.

S0188New

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.

S4353New

Terfenadine

Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

S6627New

E-4031 dihydrochloride

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

S1426

Repaglinide

Repaglinide (AG-EE 623 ZW) is a potassium channel blocker, which lowers blood glucose by stimulating the release of insulin from the pancreas, used the treatment of type II diabetes.

S2502

Quinine HCl Dihydrate

Quinine HCl Dihydrate is a white crystalline K+ channel blocker, used to treat malaria.

S1716

Glyburide (Glibenclamide)

Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.

S2443

Tolbutamide

Tolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes.

S2114

Dronedarone HCl

Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).

S2489

Nateglinide

Nateglinide (A-4166) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.

S8016

Vonoprazan Fumarate (TAK-438)

Vonoprazan Fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion. Phase 3.

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.

S2601

Gliclazide

Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.

S1715

Glipizide

Glipizide (CP-28720) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.

S6284

Tetraethylammonium bromide

Tetraethylammonium bromide is used as the source of tetraethylammonium ions in pharmacological and physiological studies, but is also used in organic chemical synthesis. It blocks selective potassium channels.

S9223

Talatisamine

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

S5371

Ajmaline

Ajmaline, found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent.

S5257

Doxapram

Doxapram is a central respiratory stimulant with a brief duration of action. Doxapram is a selective TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel inhibitor with EC50 of 410 nM, 37 μM, 9 μM, respectively.

S4037

Doxapram HCl

Doxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.

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.

S4583

Butamben

Butamben is a long-duration local anesthetic used for the treatment of chronic pain.

S6554

ML365

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

S4186

Domiphen Bromide

Domiphen bromide (NSC-39415) is a quaternary ammonium antiseptic with actions as a cationic surfactant.

S2405

Sophocarpine

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

S5028

4-Aminopyridine

4-Aminopyridine (4-AP) is a potent and non-selective inhibitor of voltage gated potassium channels (Kv) with IC50 values of 170 μM and 230 μM for Kv1.1 and Kv1.2 in CHO cells, respectively.

S8615

Sodium dichloroacetate (DCA)

Dichloroacetate, a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na+-K+-2Cl- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth.

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.

S2073

Mitiglinide Calcium

Mitiglinide Calcium is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.

S5749

Chlorpromazine

Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.

Catalog No. Information Product Use Citations Product Validations
S6559New

ML-297

ML-297 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.

S0462New

NS-1619

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

S1971

Nicorandil

Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).

S1383

Minoxidil

Minoxidil (U-10858) is a vasodilator medication known for its ability to slow or stop hair loss and promote hair regrowth. Minoxidil is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth.

S2562

Hydralazine HCl

Hydralazine HCl is a hydrochloride salt of hydralazine, which is a direct-acting smooth muscle relaxant used to treat hypertension by acting as a vasodilator primarily in arteries and arterioles.

S4630

Diazoxide

Diazoxide is a well-known small molecule that activates KATP channels in the smooth muscle of blood vessels and pancreatic beta-cells by increasing membrane permeability to potassium ions.

S4733

Retigabine

Retigabine (D-23129) is a novel anticonvulsant with activity in a broad range of seizure models. The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.

S4632

Hexachlorophene

Hexachlorophene (Hexachlorofen, Fostril, Nabac, pHisoHex) is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ± 1.29 μM; It can also attenuate Wnt/beta-catenin signaling through the Siah-1-mediated beta-catenin degradation.

S4734

Retigabine 2HCl

Retigabine is a novel anticonvulsant with activity in a broad range of seizure models. The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.

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.

Catalog No. Information Product Use Citations Product Validations
S0476New

SCH-23390 hydrochloride

SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride,SCH-23390 HCl) 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.

S0398New

Astemizole

Astemizole 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.

S3151

Gliquidone

Gliquidone is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM.