奈沙加群
- CAS号:159668-20-9
- 英文名:Napsagatran
- 中文名:奈沙加群
- CBNumber:CB01402328
- 分子式:C26H36N6O7S
- 分子量:576.67
- MOL File:159668-20-9.mol
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
奈沙加群性质、用途与生产工艺
- 生物活性 Napsagatran hydrate 是一种新型的特异性凝血酶 (thrombin) 抑制剂。
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靶点
Thrombin
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体外研究
Napsagatran (Ro 46-6240), the selective thrombin inhibitor, induces a dose-dependent prolongation of the activated partial thromboplastin time (aPTT) and prothrombin time (PT) that is evident 15 min after administration of the bolus of Napsagatran. Napsagatran also reduces the time to reperfusion in a dose-dependent manner and delays or prevents reocclusion. The decreasing intracellular amount and efflux of compound from the cells into the medium is measured. The measured CL int,efflux values are 0.13±0.06, 3.2±0.6, 10.1±2.3, and 110±2.8 for Digoxin, Fexofenadine, Napsagatran, and Rosuvastatin, respectively, thus representing drugs with a >800-fold range of efflux rates.
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体内研究
After the first hour of drug administration (from 0 to 60 min), the incorporated radioactivity into thrombi increased from baseline by 73±13, 67±22 and 32±10% in placebo, AP-1 and Napsagatran-treated rabbits, respectively. Statistical analysis confirm that thrombus growth in the placebo and AP-1 treated rabbits is not different. In contrast, reduction of 125 I-fibrinogen incorporation by Napsagatran is statistical different from the placebo group (P<0.01).
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