herg channel

ICA-105574 (ICA) is an activator of hERG that binds to the channel to remove inactivation, thus increasing peak current amplitude and shortening the action potential. It also modulates activation kinetics of the channel.

Rosuvastatin (ZD4522) is an inhibitor of HMG-CoA reductase (HMGCR) (IC50=11 nM), selective and competitive. Rosuvastatin has hypolipidemic and antiatherosclerotic effects.

Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4 and 0.8 μM).

INCB 3284 is an orally available, selective and high affinity chemokine receptor 2 (CCR2) antagonist that inhibits monocyte chemotactic protein 1 from interacting with hCCR2.INCB 3284 is used in the study of hemorrhagic shock.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator that enhances hERG currents by slowing inactivation, promoting activation, reducing inactivation, and shortening atrial and ventricular repolarization in a complex manner.

Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression.

PD-118057 is a potent ether associated (hERG) potassium channel activator that shows no activity against hERG. PD-118057 inhibits the excitability of the membrane by activating the hERG channel. PD-118057 is a potential compound for the treatment of delayed repolarization in inherited or acquired long QT syndrome and congestive heart failure.

Trk-IN-4 (PF-6683324) is a potent pan-Trk inhibitor with IC50 = 1.1~2.6 nM for TrkA/TrkB/TrkC and antinociceptive effects. It is also a selective type II PTK6 inhibitor with IC50 = 76 nM and has antitumor effects.

DA-6886 is an agonist 5-Hydroxytryptamine receptor 4 (5-HT4). DA-6886 induced relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels revealed that it inhibited hERG channel current with an pIC50 value of 4.3, indicating that the compound was 1000-fold more selective for the 5-HT4 receptor over hERG channels.

Seridopidine (ACR343) is a modulator of dopaminergic activity that is used as an oral therapy for schizophrenia, Parkinson's disease, and Tourette's syndrome.

Terodiline is a seconal amine with anticholinergic and calcium antagonistic properties that blocks the hERG current (IC50: 375 nM).Terodiline is cardiotoxic and has been used in the study of disorders caused by urethral muscle instability.

Cavutilide has antiarrhythmic activity, inhibits hERG K(+) channels, and can be used to study heart failure and persistent atrial fibrillation.

Naluzotan hydrochloride (PRX 00023 hydrochloride) is a hERG K+ channel blocker with an IC50 value of 3800 nM and is commonly used in the study of anxiety and depression.Naluzotan hydrochloride is also a novel, potent, and selective 5-HT1A agonist, with an IC50 value of about 20 nM and a Ki value of about 5.1 Naluzotan hydrochloride is also a novel, potent and selective 5-HT1A agonist with an IC50 of approximately 20 nM and a Ki of approximately 5.1 nM.

Sarizotan HCl (EMD 128130 HCl) is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinson's Dyskinesia.

Sarizotan 2HCl is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinsonian movement disorders.

Sulcardine 2HCl is a multi-ion channel blocker with antiarrhythmic effects that blocks the properties of hERG and hNav1.5 channels and can be used to study atrial fibrillation and ventricular arrhythmias.

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

Cisapride (R 51619) is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal peristalsis, increase gastric emptying and decrease esophageal reflux.

Cloperastine fendizoate (Hustazol) inhibits the hERG K+ currents in a concentration-dependent manner (IC50: 27 nM).

Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.

MCHR1 antagonist 2 is an inhibitor of melanin-concentrating hormone receptor 1 (MCH1-R, IC50 = 65 nM) and also inhibits hERG.

Betrixaban maleate is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa.

Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.