Catalog Number: 1808
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.
Background References
  1. 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.
    J.Biol.Chem., 2002;277:4989
  2. Effects of the delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit.
    Verheijck et al.
    Circ.Res., 1995;76:607
  3. Effects of the new class III antiarrhythmic drug E-4031 on myocardial contractility and electrophysiological parameters.
    Wettwer et al.
    J.Cardiovasc.Pharmacol., 1991;17:480
Citations:

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

4 Citations: Showing 1 - 4
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  1. 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
  2. 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
  3. 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
  4. Characterization of hERG1 channel role in mouse colorectal carcinogenesis.
    Authors: Fiore Et al.
    Cancer Med 2013;2:583

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