Bioactivity | 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. |
Invitro | 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]. |
In Vivo | 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]. |
Name | BMS-654457 |
CAS | 1004551-41-0 |
Formula | C36H37N5O4 |
Molar Mass | 603.71 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |