K+ channel blocker
Potent and selective blocker of the inactivating inward rectifying potassium current IKR (HERG channel). Class III antiarrythmic agent with differential atrial vs. ventricular activity.
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Product Details
Alternative Name |
4′-[[1-[2-(6-methyl-2-pyridyl)ethyl]-4-piperidinyl]carbonyl]-methanesulfonanilide |
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Appearance |
White solid. |
CAS |
113559-13-0 |
Couple Target |
HERG, Potassium channel |
Couple Type |
Blocker |
Formula |
C21H27N3O3S . 2HCl . 2H2O |
MW |
401.5 . 73.0 . 36.0 |
Purity |
≥98% (HPLC) |
Solubility |
Soluble in any aqueous buffer. Centrifuge all product preparations before use (10000 x g for 5 min). |
Handling & Storage
Use/Stability |
As indicated on product label or CoA when stored as recommended. |
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Handling |
Hygroscopic. |
Long Term Storage |
-20°C |
Shipping |
Ambient Temperature |
Regulatory Status |
RUO – Research Use Only |
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- Discovery of 1,3,4-Oxadiazole Derivatives as Broad-Spectrum Antiparasitic Agents: A. Ioana Corfu, et al.; ACS Infect. Dis. 10, 2222 (2024), Abstract
- High-Throughput Phenotypic Screening and Machine Learning Methods Enabled the Selection of Broad-Spectrum Low-Toxicity Antitrypanosomatidic Agents: Linciano, P., Quotadamo, A., et al.; J. Med. Chem. 66, 15230 (2023), Abstract
- In-vitro safety and off-target profile of the anti-parasitic arylmethylaminosteroid 1o: L. Blum, et al.; Sci. Rep. 10, 7534 (2020), Abstract — Full Text
- Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform: Moraes, C. B., Witt, G., et al.; SLAS Discov. 24, 346 (2019), Abstract
- 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 — Full Text
- A Human Induced Pluripotent Stem Cell-Derived Cardiomyocyte (hiPSC-CM) Multielectrode Array Assay for Preclinical Cardiac Electrophysiology Safety Screening: K. Harris; Curr. Protoc. Pharmacol. 71, 11.18.1 (2015), Abstract
- 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
- State dependent dissociation of HERG channel inhibitors: D. Stork, et al.; Br. J. Pharmacol. 151, 1368 (2007), Abstract
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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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