Chemical Name: N-[4-[[1-[2-(6-Methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]methanesulfonamide dihydrochloride
Biological ActivityE-4031 dihydrochloride is a selective blocker of KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr). Reversibly prolongs action potential duration in guinea pig papillary muscle and isolated ventricular myocytes, without affecting Na+ or Ca2+ inward currents. Class III antiarrhythmic agent.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations.
Ficker et al.
Effects of the new class III antiarrhythmic drug E-4031 on myocardial contractility and electrophysiological parameters.
Wettwer et al.
Effects of the delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit.
Verheijck et al.
Citations for E-4031 dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for E-4031 dihydrochloride include:
11 Citations: Showing 1 - 10
Sigma non-opioid receptor 1 is a potential therapeutic target for long QT syndrome.
Authors: Song Et al.
Neurokinin-3 receptor activation selectively prolongs atrial refractoriness by inhibition of a background K+ channel.
Authors: Veldkamp Et al.
Nat Commun 2018;9:4357
Electrophysiological measurement of ion channels on plasma/organelle membranes using an on-chip lipid bilayer system.
Authors: Kamiya Et al.
Sci Rep 2018;8:17498
An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes.
Authors: McKeithan Et al.
Front Physiol 2017;8:766
Differentiation and characterization of rhesus monkey atrial and ventricular cardiomyocytes from induced pluripotent stem cells.
Authors: Zhang Et al.
Stem Cell Res 2017;20:21
Chemical-defined and albumin-free generation of human atrial and ventricular myocytes from human pluripotent stem cells.
Authors: Pei Et al.
Stem Cell Res 2017;19:94
Ion Fluxes through KCa2 (SK) and Cav1 (L-type) Channels Contribute to Chronoselectivity of Adenosine A1 Receptor-Mediated Actions in Spontaneously Beating Rat Atria.
Authors: Bragança Et al.
Front Pharmacol 2016;7:45
Cardiac sodium/calcium exchanger preconditioning promotes anti-arrhythmic and cardioprotective effects through mitochondrial calcium-activated potassium channel.
Authors: Zhang Et al.
PLoS One 2015;8:10239
Use of Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes (hiPSC-CMs) to Monitor Compound Effects on Cardiac Myocyte Signaling Pathways.
Authors: Guo Et al.
Curr Protoc Chem Biol 2015;7:141
Apamin does not inhibit human cardiac Na+ current, L-type Ca2+ current or other major K+ currents.
Authors: Yu Et al.
Int J Clin Exp Pathol 2014;9:e96691
Characterization of hERG1 channel role in mouse colorectal carcinogenesis.
Authors: Fiore Et al.
Cancer Med 2013;2:583
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