| 货号 | 15203-50mg |
| 描述 | Voltage-gated potassium ERG channels (Kv11.1), encoded by the ether-a-go-go related gene, mediate the inwardly rectifying potassium (K+) current that repolarizes myocardial cells, gut smooth muscle cells, and interstitial cells of Cajal.1 E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM).2,3 E-4031 inhibits the ERG1, ERG2, and ERG3 isoforms with KD values of 99, 116, and 193 nM, respectively.4 However, at higher μM concentrations E-4031 can demonstrate pro-arrhythmic activity, inducing early after depolarizations (prolonged repolarization) in cell models and torsade de pointes in animal models.5 E-4031 has been used to pharmacologically rescue misprocessed ERG in long QT syndrome type 2, an autosomal dominant cardiac disease associated with prolongation of the QT interval and torsade de pointes.6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.White, E.J.,Park, S.J.,Foster, J.A., et al. Ether-a-go-go-related gene 3 is the main candidate for the E-4031-sensitive potassium current in the pacemaker interstitial cells of Cajal. American Journal of Physiology and Gastrointestinal Liver Physiology 295(4), G691-G699 (2008). 2.Jurkiewicz, N.K. and Sanguinetti, M.C. Rate-dependent prolongation of cardiac action potentials by a methanesulfonanilide class III antiarrhythmic agent. Circulation Research 72(1), 75-83 (1993). 3.Du, L.P.,Tsai, K.C.,Li, M.Y., et al. The pharmacophore hypotheses of IKr potassium channel blockers: Novel class III antiarrhythmic agents. Bioorg. Med. Chem. Lett. 14(18), 4771-4777 (2004). 4.Shi, W.,Wymore, R.S.,Wang, H.S., et al. Identification of two nervous system-specific members of the erg potassium channel gene family. Journal of Neuroscience 17(24), 9423-9432 (1997). 5.Nalos, L.,Varkevisser, R.,Jonsson, M.K., et al. Comparison of the IKr blockers moxifloxacin, dofetilide and E-4031 in five screening models of pro-arrhythmia reveals lack of specificity of isolated cardiomyocytes. British Journal of Pharmacology 165(2), 467-478 (2012). 6.Ficker, E.,Obejero-Paz, C.A.,Zhao, S., et al. The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. The Journal of Biological Chemisty 277(7), 4989-4998 (2002). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 474.4 |
| 分子式 | C21H27N3O3S • 2HCl |
| CAS号 | 113559-13-0 |
| 稳定性 | ≥ 2 years |
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