| 货号 | 15418-50mg |
| 描述 | Carvedilol is a non-selective β-antagonist with α1-adrenolytic activity that binds the α1-, α2-, and β1-adrenoceptors with Ki values of 2.2 nM, 3.4 μM, and 0.81 nM, respectively.1,2 By inhibiting excess stimulation of catecholamine it demonstrates antiarrhythmic activity in a rat model of adrenaline-induced arrhythmia with an ED50 value of 0.25 mg/kg.1 Carvedilol has also been shown to activate cardioprotective signaling through β-arrestin and ERK1/2 activation (EC50 = 2 nM).3,4,5 |
| 别名 | BM 14190;Dilatrend;SKF 105517;Talliton; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Groszek, G.,Nowak-Król, A.,Wdowik, T., et al. Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2. European Journal of Medicinal Chemistry 44(12), 5103-5111 (2009). 2.Baker, J.G. The selectivity of β-adrenoceptor antagonists at the human β1, β2 and β3 adrenoceptors. Br. J. Pharmacol. 144(3), 317-322 (2005). 3.Wisler, J.W.,DeWire, S.M.,Whalen, E.J., et al. A unique mechanism of β-blocker action: Carvedilol stimulates β-arrestin signaling. Proceedings of the Nutrition Society 104(42), 16657-16662 (2007). 4.Kim, I.M.,Tilley, D.G.,Chen, J., et al. β-blockers alprenolol and carvedilol stimulate β-arrestin-mediated EGFR transactivation. Proceedings of the National Academy of Sciences of the United States of America 105(38), 14555-14560 (2008). 5.Ibrahim, I.A.A.E.H. and Kurose, H. β-Arrestin-mediated signaling improves the efficacy of therapeutics. Journal of Pharmacological Sciences 118(4), 408-412 (2012). | |
| 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 | 406.5 |
| 分子式 | C24H26N2O4 |
| CAS号 | 72956-09-3 |
| 稳定性 | ≥ 2 years |
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