Potassium Channel

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Potassium Channel Signaling Pathway Map

Potassium Channel Signaling Pathways

Potassium Channel Products

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  • Potassium Channel Inhibitors (49)
  • Potassium Channel Activators (15)
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  • Potassium Channel Modulators (2)
  • New Potassium Channel Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
E0015New Iberiotoxin

Iberiotoxin (IbTX) is a toxin purified from the scorpion Buthus tamulus. Iberiotoxin is a potent blocker of the large conductance Ca(2+)-activated K+ channel with a Kd of ~1 nM.

E0144New Vernakalant (RSD1235) Hydrochloride

Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.

E0501New Senicapoc (ICA-17043) Senicapoc (ICA-17043) is a Gardos channel(Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM and produces dose-dependent increases in hemoglobin and decreases in markers of hemolysis. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
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).
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.
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.
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.
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.
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.
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.
Diabetes Res Clin Pract, 2022, S0168-8227(22)00588-5
Am J Cancer Res, 2020, 10(10):3302-3315
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.
Sci Rep, 2017, 7(1):3156
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.
Drug Metab Dispos, 2019, ;47(3):215-226
S1658 Dofetilide Dofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.
PLoS Pathog, 2020, 16;16(3):e1008341
Toxicol In Vitro, 2020, 104928
Clin Transl Sci, 2019, 12(6):687-697
S1715 Glipizide Glipizide (CP-28720) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.
S1716 Glyburide (Glibenclamide) Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.
PLoS Negl Trop Dis, 2021, 15(4):e0009304
Front Cell Infect Microbiol, 2021, 11:691445
Am J Transplant, 2020, 10.1111/ajt.16071
S1979 Amiodarone (NSC 85442) HCl Amiodarone (NSC 85442) HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.
Cell Rep, 2022, 38(10):110468
Front Cell Infect Microbiol, 2021, 11:630812
Drug Metab Dispos, 2020, 48(8):613-621
S2073 Mitiglinide Calcium Mitiglinide Calcium (KAD-1229) is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
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).
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
Cell Syst, 2019, 8(2):97-108
Nat Commun, 2016, 7:13023
S2405 Sophocarpine Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.
Int J Biol Sci, 2019, 15(11):2497-2508
Front Pharmacol, 2019, 10:1219
J Med Virol, 2019, 91(8):1440-1447
S2443 Tolbutamide (HLS 831) Tolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
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.
Viruses, 2022, 14(3)496
Theranostics, 2021, 11(5):2364-2380
J Colloid Interface Sci, 2021, 601:650-660
S2489 Nateglinide Nateglinide (A-4166) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
Cell Syst, 2019, 8(2):97-108
Nature, 2018, 560(7718):372-376
S2502 Quinine HCl Dihydrate Quinine HCl Dihydrate is a white crystalline K+ channel blocker, used to treat malaria.
J Pharmacol Toxicol Methods, 2017, 90:39-47
S2601 Gliclazide Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
IET Syst Biol, 2021, 10.1049/syb2.12034
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.
Mol Pain, 2019, 15:1744806919838947
Neurosci Bull, 2018, 10.1007/s12264-018-0285-8
S2967 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.
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.
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.
S4186 Domiphen Bromide Domiphen bromide (NSC-39415) is a quaternary ammonium antiseptic with actions as a cationic surfactant.
S4353 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.
S4439 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.
S4489 Tetraethylammonium chloride Tetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties.
S4495 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.
J Pharmacol Toxicol Methods, 2017, 90:39-47
S4583 Butamben Butamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain.
S4681 Quinidine hydrochloride monohydrate Quinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM.
J Biomed Res, 2021, 35(5):395-407
S5028 4-Aminopyridine 4-Aminopyridine (4-AP, Fampridine, Dalfampridine) 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.
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.
Biomed Chromatogr, 2018, 32(10)
S5371 Ajmaline Ajmaline (Cardiorythmine, Tachmalin), found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent.
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.
Pharmaceuticals (Basel), 2022, 15(2)241
Viruses, 2022, 14(3)496
Theranostics, 2021, 11(5):2364-2380
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.
S6174New NS8593 Hydrochloride NS8593 is a potent negative gating inhibitor of small conductance Ca2+ -activated K+ channels (SK1-3 or Kca2.1-2.3 channels). NS8593 is also a potent inhibitor of the TRPM7 channel with an IC50 of 1.6 µM.
S6284 Tetraethylammonium bromide Tetraethylammonium bromide (TEAB, TEA 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.
S6554 ML365 ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3).
S6627 E-4031 dihydrochloride E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type.
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.
S9223 Talatisamine Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.
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.
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.

S0050 ML277 ML277 (CID-53347902) is a potent activator of KCNQ1 channels with an EC50 of 260 nM and shows >100-fold selectivity over KCNQ2 and KCNQ4.
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.
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.
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.
Oncotarget, 2016, 7(43):69703-69717
S1971 Nicorandil Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).
BMC Cardiovasc Disord, 2021, 21(1):302
Sci Rep, 2017, 7(1):3156
J Cardiovasc Pharmacol Ther, 2016, 10.1177/1074248416636477
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.
Biogerontology, 2016, 17(5-6):907-920
Xenobiotica, 2014, 44(9):827-41
S4630 Diazoxide Diazoxide (Sch-6783, SRG-95213, Proglycem) 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.
Free Radic Biol Med, 2017, 112:616-630
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.
Toxicol Appl Pharmacol, 2022, 441:115988
Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.04.011
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.
Front Physiol, 2021, 12:790580
J Biol Chem, 2021, S0021-9258(21)00985-6
Mol Cell, 2020, S1097-2765(20)30771-1
S4734 Retigabine 2HCl Retigabine 2HCl (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.
Front Physiol, 2021, 12:790580
J Biol Chem, 2021, S0021-9258(21)00985-6
J Neurosci, 2020, 40(34):6522-6535
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.
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.
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.
E0378New PAP-1 PAP-1 (5-(4-phenoxybutoxy)psoralen), a Kv1.3 antagonist with an EC50 of 2 nM, inhibits the proliferation of human T cells and suppresses delayed type hypersensitivity in rats.
S3151 Gliquidone Gliquidone (Glurenorm) is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM.
Front Aging Neurosci, 2021, 13:754123
Front Cell Dev Biol, 2020, 8:269
Drug Test Anal, 2018, 10(3):609-617
E0034New CyPPA

CyPPA is a subtype-selective positive modulator of SK channels with EC50s of 5.6 μM and 14 μM for hSK3 and hSK2, repectively. CyPPA is inactive on both hSK1 and hIK 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.
Oxid Med Cell Longev, 2022, 2022:1733834
Biochem Biophys Res Commun, 2022, 602:135-141
Int J Mol Sci, 2021, 22(23)12878
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.
E0015New Iberiotoxin

Iberiotoxin (IbTX) is a toxin purified from the scorpion Buthus tamulus. Iberiotoxin is a potent blocker of the large conductance Ca(2+)-activated K+ channel with a Kd of ~1 nM.

E0144New Vernakalant (RSD1235) Hydrochloride

Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.

E0501New Senicapoc (ICA-17043) Senicapoc (ICA-17043) is a Gardos channel(Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM and produces dose-dependent increases in hemoglobin and decreases in markers of hemolysis. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
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).
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.
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.
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.
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.
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.
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.
Diabetes Res Clin Pract, 2022, S0168-8227(22)00588-5
Am J Cancer Res, 2020, 10(10):3302-3315
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.
Sci Rep, 2017, 7(1):3156
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.
Drug Metab Dispos, 2019, ;47(3):215-226
S1658 Dofetilide Dofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.
PLoS Pathog, 2020, 16;16(3):e1008341
Toxicol In Vitro, 2020, 104928
Clin Transl Sci, 2019, 12(6):687-697
S1715 Glipizide Glipizide (CP-28720) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.
S1716 Glyburide (Glibenclamide) Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.
PLoS Negl Trop Dis, 2021, 15(4):e0009304
Front Cell Infect Microbiol, 2021, 11:691445
Am J Transplant, 2020, 10.1111/ajt.16071
S1979 Amiodarone (NSC 85442) HCl Amiodarone (NSC 85442) HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.
Cell Rep, 2022, 38(10):110468
Front Cell Infect Microbiol, 2021, 11:630812
Drug Metab Dispos, 2020, 48(8):613-621
S2073 Mitiglinide Calcium Mitiglinide Calcium (KAD-1229) is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
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).
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
Cell Syst, 2019, 8(2):97-108
Nat Commun, 2016, 7:13023
S2405 Sophocarpine Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.
Int J Biol Sci, 2019, 15(11):2497-2508
Front Pharmacol, 2019, 10:1219
J Med Virol, 2019, 91(8):1440-1447
S2443 Tolbutamide (HLS 831) Tolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
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.
Viruses, 2022, 14(3)496
Theranostics, 2021, 11(5):2364-2380
J Colloid Interface Sci, 2021, 601:650-660
S2489 Nateglinide Nateglinide (A-4166) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
Cell Syst, 2019, 8(2):97-108
Nature, 2018, 560(7718):372-376
S2502 Quinine HCl Dihydrate Quinine HCl Dihydrate is a white crystalline K+ channel blocker, used to treat malaria.
J Pharmacol Toxicol Methods, 2017, 90:39-47
S2601 Gliclazide Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
IET Syst Biol, 2021, 10.1049/syb2.12034
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.
Mol Pain, 2019, 15:1744806919838947
Neurosci Bull, 2018, 10.1007/s12264-018-0285-8
S2967 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.
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.
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.
S4186 Domiphen Bromide Domiphen bromide (NSC-39415) is a quaternary ammonium antiseptic with actions as a cationic surfactant.
S4353 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.
S4439 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.
S4489 Tetraethylammonium chloride Tetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties.
S4495 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.
J Pharmacol Toxicol Methods, 2017, 90:39-47
S4583 Butamben Butamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain.
S4681 Quinidine hydrochloride monohydrate Quinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM.
J Biomed Res, 2021, 35(5):395-407
S5028 4-Aminopyridine 4-Aminopyridine (4-AP, Fampridine, Dalfampridine) 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.
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.
Biomed Chromatogr, 2018, 32(10)
S5371 Ajmaline Ajmaline (Cardiorythmine, Tachmalin), found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent.
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.
Pharmaceuticals (Basel), 2022, 15(2)241
Viruses, 2022, 14(3)496
Theranostics, 2021, 11(5):2364-2380
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.
S6174New NS8593 Hydrochloride NS8593 is a potent negative gating inhibitor of small conductance Ca2+ -activated K+ channels (SK1-3 or Kca2.1-2.3 channels). NS8593 is also a potent inhibitor of the TRPM7 channel with an IC50 of 1.6 µM.
S6284 Tetraethylammonium bromide Tetraethylammonium bromide (TEAB, TEA 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.
S6554 ML365 ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3).
S6627 E-4031 dihydrochloride E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type.
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.
S9223 Talatisamine Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.
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.
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.

S0050 ML277 ML277 (CID-53347902) is a potent activator of KCNQ1 channels with an EC50 of 260 nM and shows >100-fold selectivity over KCNQ2 and KCNQ4.
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.
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.
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.
Oncotarget, 2016, 7(43):69703-69717
S1971 Nicorandil Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).
BMC Cardiovasc Disord, 2021, 21(1):302
Sci Rep, 2017, 7(1):3156
J Cardiovasc Pharmacol Ther, 2016, 10.1177/1074248416636477
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.
Biogerontology, 2016, 17(5-6):907-920
Xenobiotica, 2014, 44(9):827-41
S4630 Diazoxide Diazoxide (Sch-6783, SRG-95213, Proglycem) 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.
Free Radic Biol Med, 2017, 112:616-630
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.
Toxicol Appl Pharmacol, 2022, 441:115988
Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.04.011
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.
Front Physiol, 2021, 12:790580
J Biol Chem, 2021, S0021-9258(21)00985-6
Mol Cell, 2020, S1097-2765(20)30771-1
S4734 Retigabine 2HCl Retigabine 2HCl (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.
Front Physiol, 2021, 12:790580
J Biol Chem, 2021, S0021-9258(21)00985-6
J Neurosci, 2020, 40(34):6522-6535
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.
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.
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.
E0378New PAP-1 PAP-1 (5-(4-phenoxybutoxy)psoralen), a Kv1.3 antagonist with an EC50 of 2 nM, inhibits the proliferation of human T cells and suppresses delayed type hypersensitivity in rats.
S3151 Gliquidone Gliquidone (Glurenorm) is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM.
Front Aging Neurosci, 2021, 13:754123
Front Cell Dev Biol, 2020, 8:269
Drug Test Anal, 2018, 10(3):609-617
E0034New CyPPA

CyPPA is a subtype-selective positive modulator of SK channels with EC50s of 5.6 μM and 14 μM for hSK3 and hSK2, repectively. CyPPA is inactive on both hSK1 and hIK 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.
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.
E0015New Iberiotoxin

Iberiotoxin (IbTX) is a toxin purified from the scorpion Buthus tamulus. Iberiotoxin is a potent blocker of the large conductance Ca(2+)-activated K+ channel with a Kd of ~1 nM.

E0144New Vernakalant (RSD1235) Hydrochloride

Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.

E0501New Senicapoc (ICA-17043) Senicapoc (ICA-17043) is a Gardos channel(Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM and produces dose-dependent increases in hemoglobin and decreases in markers of hemolysis. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
S6174New NS8593 Hydrochloride NS8593 is a potent negative gating inhibitor of small conductance Ca2+ -activated K+ channels (SK1-3 or Kca2.1-2.3 channels). NS8593 is also a potent inhibitor of the TRPM7 channel with an IC50 of 1.6 µM.
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.

E0378New PAP-1 PAP-1 (5-(4-phenoxybutoxy)psoralen), a Kv1.3 antagonist with an EC50 of 2 nM, inhibits the proliferation of human T cells and suppresses delayed type hypersensitivity in rats.
E0034New CyPPA

CyPPA is a subtype-selective positive modulator of SK channels with EC50s of 5.6 μM and 14 μM for hSK3 and hSK2, repectively. CyPPA is inactive on both hSK1 and hIK channels.