达比加群酯
CAS号 | 211915-06-9 | 货号 | BCP02864 |
中文名 | 达比加群酯 | ||
英文名 | Dabigatran etexilate | ||
中文别名 | |||
英文别名 | Prazaxa;BIBR 1048;BIBR-1048;BIBR1048; | ||
分子式 | C34H41N7O5 | 分子量 | 627.73 |
生物活性 | Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran inhibits thrombin generation in platelet-poor plasma (PPP) with IC50 of 0.56 μM, measured as the endogenous thrombin potential (ETP). Dabigatran demonstrates concentrationdependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 μM, respectively. | ||
信号通路 | Protease/Metabolic Enzyme | ||
靶 点 | Thrombin |
结构式
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