E-4031 dihydrochloride

Cat. No. 1808

E-4031 dihydrochloride C21H27N3O3S.2HCl [113559-13-0]

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Chemical Name: N-[4-[[1-[2-(6-Methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]methanesulfonamide dihydrochloride

Biological Activity

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.

Technical Data

M.Wt:
474.44
Formula:
C21H27N3O3S.2HCl
Solubility:
Soluble to 100 mM in water and to 50 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
113559-13-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Ficker et al (2002) The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. J.Biol.Chem. 277 4989. PMID: 11741928.

Verheijck et al (1995) Effects of the delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit. Circ.Res. 76 607. PMID: 7895335.

Wettwer et al (1991) Effects of the new class III antiarrhythmic drug E-4031 on myocardial contractility and electrophysiological parameters. J.Cardiovasc.Pharmacol. 17 480. PMID: 1711611.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for E-4031 dihydrochloride include:

Guo et al (2015) Use of Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes (hiPSC-CMs) to Monitor Compound Effects on Cardiac Myocyte Signaling Pathways. Curr Protoc Chem Biol 7 141. PMID: 26331525.

Zhang et al (2015) Cardiac sodium/calcium exchanger preconditioning promotes anti-arrhythmic and cardioprotective effects through mitochondrial calcium-activated potassium channel. PLoS One 8 10239. PMID: 26617732.

Yu et al (2014) Apamin does not inhibit human cardiac Na+ current, L-type Ca2+ current or other major K+ currents. Int J Clin Exp Pathol 9 e96691. PMID: 24798465.

Fiore et al (2013) Characterization of hERG1 channel role in mouse colorectal carcinogenesis. Cancer Med 2 583. PMID: 24403225.

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Keywords: E-4031 dihydrochloride, supplier, HERG, KV11.1, channel, blockers, inhibits, inhibitors, rapid, delayed, rectifier, K+, current, IKr, Potassium, KV, Channels, Human, Ether-A-Go-Go, Gene, voltage-gated, voltage-dependent, Tocris Bioscience, Voltage-gated Potassium (KV) Channel Blocker products

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