BMS-654457 |
カタログ番号GC32614 |
BMS-654457 は、小分子の第 XIa 因子 (FXIa) の可逆的阻害剤であり、それぞれ 0.2 および 0.42 nM の Kis でヒトおよびウサギの FXIa と結合します。
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Cas No.: 1004551-41-0
Sample solution is provided at 25 µL, 10mM.
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.
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[1].
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[1].
[1]. Wong PC, et al. In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa. J Thromb Thrombolysis. 2015 Nov;40(4):416-23.
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