| 货号 | 15213-500mg |
| 描述 | Amiodarone is a class III antiarrhythmic agent, in that it prolongs both cardiac action potential and refractoriness by blocking potassium currents.1 It inhibits the voltage-gated potassium channel hERG, also known as KCNH2, with an IC50 value of 1 µM.2 In addition, amiodarone binds with high affinity to the sigma-1 opioid receptor, 3-β-hydroxysteroid Δ8Δ7 isomerase, and C-8 sterol isomerase (Kis = 1, 25, and 62 nM, respectively) and inhibits human thyroid hormone receptors α and β (IC50s = 0.6, 0.65 µM, respectively).3,4 It also inhibits the cytochrome P450 (CYP) isoforms CYP2C8 and CYP3A4 in vitro at low micromolar concentrations.5 |
| 别名 | Cordarex;Pacerone®; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Campbell, T.J. and Williams, K.M. Therapeutic drug monitoring: Antiarrhythmic drugs. British Journal of Clinical Pharmacology 46, 307-319 (1998). 2.Sinha, N. and Sen, S. Predicting hERG activities of compounds from their 3D structures: Development and evaluation of a global descriptors based QSAR model. European Journal of Medicinal Chemistry 46(2), 618-630 (2011). 3.Laggner, C.,Schieferer, C.,Fiechtner, B., et al. Discovery of high-affinity ligands of σ1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening. Journal of Medicinal Chemistry 48(15), 4754-4764 (2005). 4.Carlsson, B.,Singh, B.N.,Temciuc, M., et al. Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone. Journal of Medicinal Chemistry 45(3), 623-630 (2002). 5.Polasek, T.M.,Elliott, D.J.,Lewis, B.C., et al. Mechanism-based inactivation of human cytochrome P4502C8 by drugs in vitro. Journal of Pharmacology and Experimental Therapeutics 311(3), 996-1007 (2004). | |
| 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 | 681.8 |
| 分子式 | C25H29I2NO3 • HCl |
| CAS号 | 19774-82-4 |
| 稳定性 | ≥ 2 years |
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