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:
10 Citations: Showing 1 - 10
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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A representative action potential of a guinea pig cardiomyocyte before and after perfusion with 500 nM E-4031 for 5 min and stimulated at a frequency of 1 Hz in a whole cell patch clamp model. E-4031 significantly shortened action potential duration of guinea pig ventricular cardiomyocytes.
As an antiarrhythmic drug E-4031 was studied to identify drug effect. Concentration dependent Kv channel blocking and control of release were studied. The compound showed blocking activity which is not dependent on concentration administered and data was reproducible. Great product stability and dissolves nicely.