Letaxaban
| CAS号 | 870262-90-1 | 货号 | BCP24734 |
| 中文名 | Letaxaban | ||
| 英文名 | Letaxaban | ||
| 中文别名 | |||
| 英文别名 | TAK 442; TAK442;TAK-442; | ||
| 分子式 | C22H26ClN3O5S | 分子量 | 479.98 |
| 生物活性 | Letaxaban, also known as TAK-442, is a potent, selective, and orally active factor Xa inhibitor, which is a tetrahydropyrimidin-2(1H)-one derivative. TAK-442 inhibited endogenous FXa activity in platelet-poor human [half-maximal inhibitory concentration (IC(50)): 53 nM, TAK-442 ] and rat (IC(50): 32 nM, TAK-442 ) plasma. TAK-442 inhibited in vitro reconstituted human prothrombinase (system included FXa, calcium, and washed platelets) with an IC(50) value of 51 nM. In a rat model of balloon injury, thrombin activity on the surface of injured vessels increased to 3.2-, 22-, and 5.8-fold the activity on the surface of the intact aorta at 5 minutes, 1 hour, and 24 hours after the injury, respectively. At approximately 1 hour after the injury, TAK-442 blocked platelet-associated thrombin generation on the surface of injured aortas with an IC(50) value of 19 nM. (source: J Cardiovasc Pharmacol. 2011 Feb;57(2):201-6.) | ||
| 信号通路 | Protease/Metabolic Enzyme | ||
| 靶 点 | Factor Xa | ||
结构式
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