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编 号:F002549
分子式:C36H37N5O4
分子量:603.71
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生物活性:
BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa), binding with human and rabbit FXIa with Kis of 0.2 and 0.42 nM, respectively.

体内研究:
BMS-654457 is effective in the prevention of arterial thrombosis in rabbits with limited effects on bleeding time. BMS-654457 is a promising antithrombotic therapy with a wide therapeutic window.

体外研究:
BMS-654457 shows comparable in vitro potency against FXIa in humans (Ki=0.2 nM) and in rabbits (Ki =0.42 nM), and was over 500-fold selective against coagulation-related proteases (thrombin, FXa and FVIIa) in these species.
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