BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa , with an IC 50 of 2.8 nM against human factor XIa. BMS-262084 also inhibits human tryptase ( IC 50 =5 nM). BMS-262084 exhibits antithrombotic effects In Vitro BMS-262084 shows more than 70-fold selectivity for human factor XIa (IC 50 =2.8 nM) over tryptase, trypsin, urokinase, plasma kallikrein, plasmin, yhrombin (factor IIa) and Factor IXa (IC 50 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague Dawley rats (310-390 g) were induced venous thrombosis by FeCl 2 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 FeCl 2 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. Form:Solid IC50& Target:IC50: 2.8 nM (factor XIa), 5 nM (tryptase)
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BMS-262084
CAS number：253174-92-4 molecular formula：C18H31N7O5
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| Chinese alias | - | ||
| English alias | 2-Azetidinecarboxylic acid, 3-(3-((aminoiminomethyl)amino)propyl)-1-((4-(((1,1-dimethylethyl)amino)carbonyl)-1-piperazinyl)carbonyl)-4-oxo-, (2S,3R)- | BDBM50120368 | (3S,4R)-1-(4-tert-Butylcarbamoyl-piperazine-1-carbonyl)-3-(3-guanidino-propyl)-4-oxo-aze | ||
| CAS number | 253174-92-4 | molecular formula | C18H31N7O5 |
| molecular weight | 425.48 g/mol | Exact mass | ≥98% |
| PSA | 175.000 Ų | logp | -1.9 |
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