A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception[1].
MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM.
Minoxidil-d10 (U10858-d10) is the deuterium labeled Minoxidil. Minoxidil (U10858) is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC50 of 20 μM[1][2][3].
Alloisolithocholic acid (AILCA) activates large-conductance calcium-activated potassium (BK) channels with an EC50 value of 44.21 μM in Xenopus oocytes[1].
Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons[1][2].
DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC50 of 4.9 µM. DPP-4/GPR119 modulator 1 can be used for diabetes research[1][1].
LY 97241 accelerates the apparent rate of inactivation of transient outward K current. LY 97241 is an antiarrhythmic drug[1].
Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase[1][2][3].
ML252 is a selective inhibitor of potassium channel, targeting to KCNQ2 channel (Kv7.2) (IC50=69 nM). ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively[1][2].
Phrixotoxin 1, from the venom of the theraphosid spider Phrixotrichus auratus, is a specific peptide inhibitor of Kv4 potassium channel[1][2].
Mitiglinide(KAD-1229; S21403) is a drug for the treatment of type 2 diabetes; it is a highly selective KATP channel antagonist. IC50 value:Target: KATP channelMitiglinide is a hypoglycemic agent that closes adenosine triphosphate (ATP)-sensitive potassium channels (KATP channel s) in the pancreatic β-islet cells. Mitiglinide stimulates insulin secretion by stimulating Ca2+ influx.
WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. WX-081 exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for drug susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. WX-081 also inhibits hERG channel with the IC50 of 1.89 μM[1].
NS309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels); increases Ca2+ sensitivity. Displays no activity at BK channels.IC50 value: Ca2+-activated K+ channelTarget:
KV2 channel inhibitor-1 is a selective KV2 channel inhibitor with IC50s of 0.2 μM and 0.41 μM for KV2.1 and KV2.2, respectively. KV2 channel inhibitor-1 possesses good selectivity over KV1.2 (IC50>10 μM). KV2 channel inhibitor-1 is >10-fold selective over NaV channels and other KV channels and displays weak activity on CaV channels[1].
Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM[1]. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo[2].
Dimethyl L-glutamate (Dimethyl glutamate), a membrane-permeable analog of Glutamate, can stimulate insulin release induced by Glucose. Dimethyl L-glutamate suppresses the KATP channel activities. Dimethyl L-glutamate inhibits E. gracilis growth and causes abnormal cell division. Dimethyl L-glutamate can be used in the research of diabetes, glucose transport, phosphorylation, and further metabolism[1][2][3][4].
Diazoxide-d3 is deuterium labeled Diazoxide. Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.
Tipepidine reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine subsequently activates VTA dopamine neuron[1]. Tipepidine, a non-narcotic antitussive, exerts an antidepressant-like effect[2].
BMS-191095 is an activators of mitochondrial ATP-sensitive potassium (mitoKATP) channels.Target: potassium channelin vitro: BMS-191095 induces mitochondrial-depolarization and vasodilation. BMS-191095 elicites a dose-dependent vasodilation in endothelium denuded cerebral arteries with 8.1 ± 2.3%, 31.6 ± 2.1%, and 39.5 ± 3.2% relaxation in response to 10, 50, and 100 μM, respectively. in vivo: In normal rats, BMS-191095-induced vasodilation was mediated by mitochondrial depolarization and calcium sparks generation in VSM and was reduced by inhibition of BKCa channels.
Spinoxin isolated from the venom of scorpion Heterometrus spinifer, is a 34-residue peptide neurotoxin cross-linked by four disulfide bridges. Spinoxin is a potent inhibitor of Kv1.3 potassium channel (IC50 = 63 nM), considering to be valid molecular targets in the diagnostics and therapy of various autoimmune disorders and cancers[1].
Kv3 modulator 2 (formula (I)) is a potent Kv3 channels modulator extracted from patent WO2018109484A1, compound formula (I) , has analgesic activity and is used in the prophylaxis or treatment of related disorders[1].
VU591 hydrochloride is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM[1].
Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM. Target: Potassium ChannelAmiodarone shows beta blocker-like and potassium channel blocker-like actions on the SA and AV nodes, increases the refractory period via sodium- and potassium-channel effects, and slows intra-cardiac conduction of the cardiac action potential, via sodium-channel effects. Amiodarone (2-butyl, 3-(4-diethylaminoethoxy, 3,5-diiodo, benzoyl) benzofuran hydrochloride), an anti-anginal drug which causes coronary dilatation and depresses myocardial oxygen consumption, was found to protect anaesthetized guinea-pigs against ouabain-induced ventricular fibrillation.2. A 5% (73.4 mM) solution of amiodarone had no local anaesthetic action on guinea-pig skin [1]. Amiodarone proved safe in patients with severe congestive heart failure and severe myocardial damage. Its clinical efficacy was related to its electrophysiologic properties and to two unique properties: its wide safety margin and its cumulative effect [2].
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV[1].
Budiodarone (ATI-2042) tartrate is a chemical analogue of Amiodarone (HY-14187) with balanced, multiple cardiac ion channel (potassium, sodium and calcium channels) inhibiting activity. Budiodarone tartrate is an antiarrhythmic agent[1].
LY303511 is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K+ currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
NS19504 is a Ca2+-activated K+ channel (BK channel, KCa1.1 channel) activator (EC50=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions[1].
VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM[1].
YM758 is a “funny” If current channel (If channel) inhibitor.