产品
编 号:F715547
分子式:C18H31N7O5
分子量:425.48
产品类型
结构图
CAS No: 253174-92-4
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产品详情
生物活性:
BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa, with an IC50 of 2.8 nM against human factor XIa. BMS-262084 also inhibits human tryptase (IC50=5 nM). BMS-262084 exhibits antithrombotic effects.
体内研究:
BMS-262084 (2-12 mg/kg + 2-12 mg/kg/h; i.v.) reduces carotid artery thrombus weight and improves both vessel patency and integrated flow in rats.Animal Model:Male Sprague Dawley rats (310-390 g) were induced venous thrombosis by FeCl2
Dosage:2 mg/kg + 2 mg/kg/h, 6 mg/kg + 6 mg/kg/h, 12 mg/kg + 12 mg/kg/h
Administration:I.v. 10 min before FeCl2 application
Result:Reduced carotid artery thrombus weight by 73% at the dose of 12 mg/kg + 12 mg/kg/h.Improved both vessel patency and integrated flow.
体外研究:
BMS-262084 shows more than 70-fold selectivity for human factor XIa (IC50=2.8 nM) over tryptase, trypsin, urokinase, plasma kallikrein, plasmin, yhrombin (factor IIa) and Factor IXa (IC50=0.005, 0.05, 0.542, 0.55, 1.7,10.5, and 17.4 μM, respectively).BMS-262084 (1-100 μM) doubles the activated thromboplastin time in human and rat plasma at 0.14 and 2.2 μM, respectively.