| DC45198 |
Lei-Dab7 |
Lei-Dab7 is a high affinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. |
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| DC45323 |
Nifekalant hydrochloride |
Nifekalant hydrochloride (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC50 of 10 µM. Nifekalant hydrochloride can be used for refractory ventricular tachyarrhythmias research. |
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| DC45580 |
Levosimendan D3 |
Levosimendan D3 (Simsndan D3) is a deuterium labeled Levosimendan. Levosimendan is a calcium sensitiser used in the management of acutely decompensated congestive heart failure. |
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| DC45784 |
UCL 1684 dibromide |
UCL 1684 (dibromide) is a first nanomolar, non-peptidic small conductance calcium-activated potassium (SK) channel blocker. UCL 1684 (dibromide) is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of INa. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness. |
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| DC46296 |
Gliclazide (D4) |
Gliclazide D4 (S1702 D4) is the deuterium labeled Gliclazide. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic. |
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| DC46366 |
ICA-105665 |
ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects. |
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| DC46509 |
Cesium chloride |
Cesium chloride is a blocker of potassium channel. Cesium chloride prevents the decrease of Na+ transport produced by Alloxan. Cesium chloride has induced cardiac arrhythmias, including torsade de pointes in animal models. |
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| DC46518 |
DAD dichloride |
DAD dichloride is a type of ion channel blocker that blocks voltage-gated potassium channels. DAD dichloride is a third-generation photoswitch that responds to visible light. DAD dichloride has the potential for restoring visual function. |
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| DC46519 |
DAD |
DAD is a type of ion channel blocker that blocks voltage-gated potassium channels. DAD is a third-generation photoswitch that responds to visible light. DAD has the potential for restoring visual function. |
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| DC46591 |
BeKm-1 TFA |
BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart. |
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| DC47244 |
Iptakalim hydrochloride |
Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist. |
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| DC47375 |
Guangxitoxin 1E |
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. |
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| DC47376 |
Rimtuzalcap
Featured
|
Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA). |
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| DC47930 |
OSK-1 |
OSK-1 is a potent Kv channel blocker with IC50s of of 0.6 nM, 5.4 nM, 0.014 nM for Kv1.1, Kv1.2 and Kv1.3, respectively. OSK1 is a moderate blocker of Ca2+-activated KCa3.1 channel with an IC50 of 225 nM. OSK-1 belongs to α-KTx3 toxins and is used as a immunosuppressive drug. |
|
| DC48199 |
Isoallolithocholic acid |
Alloisolithocholic acid (AILCA) activates large-conductance calcium-activated potassium (BK) channels with an EC50 value of 44.21 μM in Xenopus oocytes. |
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| DC48200 |
Cibenzoline |
Cibenzoline is a potent inhibitor of KATP channel with directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline is a class Ia antiarrhythmic drug. Cibenzoline has little anticholinergic activity. Cibenzoline markedly attenuate LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for the research of hypertrophic obstructive cardiomyopathy. |
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| DC48583 |
Pinacidil |
Pinacidil is a potent activator of potassium channel. Pinacidil is an antihypertensive agent which hyperpolarises vascular smooth muscle by opening K+-channels. Pinacidil significantly improves the reperfusion function and cardiac compliance. Pinacidil has direct cardioprotective efficacy. |
|
| DC48637 |
Tipepidine |
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. Tipepidine, a non-narcotic antitussive, exerts an antidepressant-like effect. |
|
| DC48641 |
Chromanol 293B |
Chromanol 293B is a selective blocker of the slow delayed rectifier K+ current (IKs) with IC50 of 1-10 μM and a weak inhibitor of KATP channel. Chromanol 293B also blocks the CFTR chloride current with an IC50 of 19 μM. |
|
| DC48749 |
Clamikalant sodium |
Clamikalant sodium (HMR 1098) is an ATP-sensitive potassium (KATP) channel blocker. Clamikalant sodium can be used for the research of arrhythmia. |
|
| DC48873 |
DPO-1
Featured
|
DPO-1 is a potent inhibitor of the voltage-gated potassium channel subtype Kv1.5 and a blocker of ultrarapid delayed rectifier potassium current. DPO-1 prevents atrial arrhythmia. |
|
| DC49706 |
KCa2 channel modulator 2 |
KCa2 channel modulator 2 (compound 2q) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 2 exhibits similar potency on the rat KCa2.2a and human KCa2.3 channel subtypes, with EC50s of 0.64 μM and 0.60 μM, respectively |
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| DC49707 |
KCa2 channel modulator 1 |
KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 1 potentiates human KCa2.3 channels with an EC50 value of 0.19 μM and 0.99 μM on the rat KCa2.2 channel subtype. |
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| DC49708 |
QO 58 |
QO 58 is a potent modulator of K(v)7 channels. QO-58 increases the current amplitudes, shifts the voltage-dependent activation curve in a more negative direction and slows the deactivation of K(v)7.2/K(v)7.3 currents. QO-58 has the potential for the research of diseases associated with neuronal hyperexcitability. |
|
| DC49709 |
Linoleoyl glycine |
Linoleoyl glycine is a modified polyunsaturated fatty acid. Linoleoyl glycine has activating effects on human KCNQ1/KCNE1 (hKCNQ1/hKCNE1) channels expressed in Xenopus oocytes. |
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| DC70143 |
SB-335573 |
A potent, selective hERG potassium channel (Kv11.1) activator. |
|
| DC70158 |
A293 |
A293 (AVE1231) is a potent and antiarrhythmic compound and selective inhibitor of two-pore-domain potassium channel TASK-1 (KCNK3, hK2P3.1).A293 (AVE1231) is an inhibitor of hKv1.5 currents with predominant action on channels in their open state.A293 (1 uM) prominently depolarized arterial smooth muscle and increased basal tone level and contractile responses to methoxamine of arteries from young rats but had almost no effect in adult rats.Pharmacological inhibition of atrial TASK-1 currents via A293 (AVE1231) exerts antiarrhythmic effects in vivo as well as in silico, resulting in acute cardioversion of paroxysmal trial fibrillation (AF). |
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| DC70245 |
Benzopyran-G1 |
Benzopyran-G1 is a selective inhibitor of cardiac acetylcholine-activated inwardly rectifying K+ current (IKACh), composed of Kir3.1/Kir3.4 heterotetrameric and Kir3.4 homotetrameric channel subunits. |
|
| DC70327 |
CTIBD
Featured
|
CTIBD is a novel potent activator of the BKCa channel with EC50 of 3.9 uM.CTIBD showed significantly higher potency compared with three other known BKCa activators: NS 1619, NS 11021, and rottlerin.CTIBD induced a reversible potentiation of macroscopic outward currents of the BKCa channel, CTIBD activates both rSlo/rβ1 and rSlo/rβ4 coexpressed channels mainly by decreasing the closing rate of the channel.CTIBD concentration-dependently reduced ACh-induced contractions in isolated rat urinary bladder strips. CTIBD effectively restored frequent voiding contraction and lowered voiding volume without affecting other bladder function parameters in acetic acid-induced overactive bladder (OAB) model (i.p. 20 mg/kg). |
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| DC70426 |
GAT1508
Featured
|
GAT1508 (GAT-1508) is a potent, specific activator for brain-expressed GIRK1/2 channels (EC50=75 nM), specifically activates the brain GIRK1/2 over the cardiac GIRK1/4;
GAT1508 is an allosteric modulator of channel–phosphatidylinositol 4,5-bisphosphate interactions.
GAT1508 effectively extinguished conditioned fear in rodents and lacked cardiac and behavioral side effects, suggesting its potential for use in pharmacotherapy for post-traumatic stress disorder. |
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