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
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S1715 |
Glipizide
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Glipizide (CP-28720) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes. |
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S1716 |
Glyburide (Glibenclamide)
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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
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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
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S2073 |
Mitiglinide Calcium
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Mitiglinide Calcium (KAD-1229) is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells. |
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S2114 |
Dronedarone HCl
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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
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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
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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
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S2456 |
Chlorpromazine HCl
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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
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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
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S2502 |
Quinine HCl Dihydrate
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Quinine HCl Dihydrate is a white crystalline K+ channel blocker, used to treat malaria. |
- J Pharmacol Toxicol Methods, 2017, 90:39-47
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S2601 |
Gliclazide
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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
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S2825 |
ML133 HCl
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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
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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. |
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S3242 |
Loureirin B
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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. |
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S4037 |
Doxapram HCl
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Doxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively. |
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S4186 |
Domiphen Bromide
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Domiphen bromide (NSC-39415) is a quaternary ammonium antiseptic with actions as a cationic surfactant. |
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S4353 |
Terfenadine
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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. |
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S4439 |
Almitrine mesylate
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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. |
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S4489 |
Tetraethylammonium chloride
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Tetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties. |
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S4495 |
Quinine
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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
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S4583 |
Butamben
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Butamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain. |
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S4681 |
Quinidine hydrochloride monohydrate
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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
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S5028 |
4-Aminopyridine
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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. |
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S5257 |
Doxapram
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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)
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S5371 |
Ajmaline
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Ajmaline (Cardiorythmine, Tachmalin), found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent. |
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S5749 |
Chlorpromazine
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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
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S5773 |
NS1643
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NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents. |
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S6174New |
NS8593 Hydrochloride
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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. |
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S6284 |
Tetraethylammonium bromide
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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. |
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S6554 |
ML365
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ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3). |
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S6627 |
E-4031 dihydrochloride
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E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type. |
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S8016 |
Vonoprazan Fumarate (TAK-438)
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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. |
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S9223 |
Talatisamine
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Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities. |
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S9251 |
Oxypeucedanin
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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. |
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E0030New |
NS309
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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.
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S0050 |
ML277
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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. |
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S0144 |
ICA 069673
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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. |
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S0462 |
NS-1619
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NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels. |
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S0467 |
Emodepside
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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. |
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S1383 |
Minoxidil
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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
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S1971 |
Nicorandil
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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
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S2562 |
Hydralazine HCl
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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
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S4630 |
Diazoxide
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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
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S4632 |
Hexachlorophene
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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
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S4733 |
Retigabine
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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
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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
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S6553 |
ML213
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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. |
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S6559 |
ML-297
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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. |
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S6572 |
ML335
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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. |
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