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E-4031 . dihydrochloride

K+ channel blocker
BML-KC158-0005 5 mg 170.00 USD
BML-KC158-0025 25 mg 667.00 USD
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Replaces Prod. #: ALX-430-111

Potent and selective blocker of the inactivating inward rectifying potassium current IKR (HERG channel). Class III antiarrythmic agent with differential atrial vs. ventricular activity.

Product Specification

Alternative Name:4'-[[1-[2-(6-methyl-2-pyridyl)ethyl]-4-piperidinyl]carbonyl]-methanesulfonanilide
Formula:C21H27N3O3S . 2HCl . 2H2O
MW:401.5 . 73.0 . 36.0
Purity:≥98% (HPLC)
Appearance:White solid.
Solubility:Soluble in water (100mg/ml) or DMSO.
Long Term Storage:Ambient
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Product Literature References

Characterization of the effects of Ryanodine, TTX, E-4031 and 4-AP on the sinoatrial and atrioventricular nodes: M.R. Nikmaram, et al.; Prog. Biophys. Mol. Biol. 96, 452 (2008), Abstract;
Pharmacological and biophysical isolation of K+ currents encoded by ether-à-go-go-related genes in murine hepatic portal vein smooth muscle cells: S.Y. Yeung & I.A. Greenwood; Am. J. Physiol. Cell Physiol. 292, C468 (2007), Abstract; Full Text
Role of reverse mode Na+/Ca2+ exchanger in the cardioprotection of metabolic inhibition preconditioning in rat ventricular myocytes: S.Z. Liu, et al.; Eur. J. Phamacol. 561, 14 (2007), Abstract;
State dependent dissociation of HERG channel inhibitors: D. Stork, et al.; Br. J. Pharmacol. 151, 1368 (2007), Abstract;
Molecular determinants of HERG channel block: K. Kamiya, et al.; Mol. Pharmacol. 69, 1709 (2006), Abstract; Full Text
Postnatal development of E-4031-sensitive potassium current in rat carotid chemoreceptor cells: I. Kim, et al.; J. Appl. Physiol. 98, 1469 (2005), Abstract; Full Text
A rapidly activating delayed rectifier K+ current regulates pacemaker activity in adult mouse sinoatrial node cells: R.B. Clark, et al.; Am. J. Physiol. Heart Circ. Physiol. 286, H1757 (2004), Abstract; Full Text
Contribution of IKr to rate-dependent action potential dynamics in canine endocardium: F. Hua & R.F. Gilmour Jr.; Circ. Res. 94, 810 (2004), Abstract; Full Text
Expression and role of the ether-à-go-go-related (MERG1A) potassium-channel protein during preimplantation mouse development: N.J. Winston, et al.; Biol. Reprod. 70, 1070 (2004), Abstract; Full Text
Single-channel recordings of a rapid delayed rectifier current in adult mouse ventricular myocytes: basic properties and effects of divalent cations: G.X. Liu; J. Physiol. 556, 401 (2004), Abstract; Full Text
Expression and function of KCNH2 (HERG) in the human jejunum: A.M. Farrelly; Am. J. Physiol. Gastrointest. Liver Physiol. 284, G883 (2003), Abstract; Full Text
E-4031 enhanced Ca2+ transient and ventricular myocytes contraction via reverse mode Na+/Ca2+ exchange in normal and hypertrophic rats: X.L Cui, et al.; Acta Pharmacol. Sin. 23, 797 (2002), Abstract;
Functional up-regulation of HERG K+ channels in neoplastic hematopoietic cells: G.A. Smith, et al.; J. Biol. Chem. 277, 18528 (2002), Abstract; Full Text
Differential atrial versus ventricular activities of class III potassium channel blockers.: E.P. Baskin & J.J. Lynch; J. Pharmacol. Exp. Therap. 285, 135 (1998), Abstract;
Effects of divalent cations on the E-4031-sensitive repolarization current, I(Kr), in rabbit ventricular myocytes: T. Paquette, et al.; Biophys. J. 74, 1278 (1998), Abstract; Full Text
Modulation of HERG affinity for E-4031 by [K+]o and C-type inactivation: S. Wang, et al.; FEBS Lett. 417, 43 (1997), Abstract;
The class III antiarrhythmic agent E-4031 selectively blocks the inactivating inward-rectifying potassium current in rat anterior pituitary tumor cells (GH3/B6 cells): F. Weinsberg et al.; Pflugers Arch. 434, 1 (1997), Abstract;
Effects of class III antiarrhythmic drugs on the Na(+)-activated K+ channels in guinea-pig ventricular cells: K. Mori, et al.; Br. J. Pharmacol. 119, 133 (1996), Abstract;
Inhibition of potassium currents by the antiarrhythmic drug E4031 in rat taste receptor cells: X.D Sun & M.S. Herness; Neurosci. Lett. 204, 149 (1996), Abstract;
Differential class III and glibenclamide effects on action potential duration in guinea-pig papillary muscle during normoxia and hypoxia/ischaemia: I. MacKenzie, et al.; Br. J. Pharmacol. 110, 531 (1993), Abstract; Full Text
Effects of antiarrhythmic agents classified as class III group on ischaemia-induced myocardial damage in canine hearts: T. Sano, et al.; Br. J. Pharmacol. 99, 577 (1990), Abstract; Full Text

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