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 Details
| Alternative Name: | 4'-[[1-[2-(6-methyl-2-pyridyl)ethyl]-4-piperidinyl]carbonyl]-methanesulfonanilide |
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| Formula: | C21H27N3O3S . 2HCl . 2H2O |
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| MW: | 401.5 . 73.0 . 36.0 |
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| CAS: | 113559-13-0 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | White solid. |
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| Solubility: | Soluble in any aqueous buffer. Centrifuge all product preparations before use (10000 x g for 5 min). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Handling: | Hygroscopic. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
In-vitro safety and off-target profile of the anti-parasitic arylmethylaminosteroid 1o: L. Blum, et al.; Sci. Rep.
10, 7534 (2020),
Abstract;
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Contractions of Human-iPSC-derived Cardiomyocyte Syncytia Measured with a Ca-sensitive Fluorescent Dye in Temperature-controlled 384-well Plates: C. Forny, et al.; J. Vis. Exp.
140, 58290 (2018),
Abstract;
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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;
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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;
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Postnatal development of E-4031-sensitive potassium current in rat carotid chemoreceptor cells: I. Kim, et al.; J. Appl. Physiol.
98, 1469 (2005),
Abstract;
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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;
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Contribution of IKr to rate-dependent action potential dynamics in canine endocardium: F. Hua & R.F. Gilmour Jr.; Circ. Res.
94, 810 (2004),
Abstract;
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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;
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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;
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Expression and function of KCNH2 (HERG) in the human jejunum: A.M. Farrelly; Am. J. Physiol. Gastrointest. Liver Physiol.
284, G883 (2003),
Abstract;
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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;
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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;
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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;
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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;
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