BMS-593214 is an active-site, direct FVIIa inhibitor. BMS-593214 displayed direct, competitive inhibition of human FVIIa in the hydrolysis of a tripeptide substrate with Ki of 5 nM. However, it acted as a noncompetitive inhibitor of the activation of the physiological substrate FX by TF/VIIa with Ki of 9.3 nM. BMS-593214 showed selectivity for FVIIa and exhibited species differences in TF-FVIIa-dependent anticoagulation with similar potency in human and rabbit plasma. BMS-593214 was efficacious in the prevention and treatment models of AT and VT with ED50 values of 1.1 to 3.1 mg/kg. Furthermore, BMS-593214 exhibited a wide therapeutic window with respect to BT. These results suggest that inhibition of FVIIa with small-molecule active-site inhibitors represents a promising antithrombotic approach for the development of new therapies for the prevention and treatment of AT and VT. References: Priestley ES, De Lucca I, Zhou J, Zhou J, Saiah E, Stanton R, Robinson L, Luettgen JM, Wei A, Wen X, Knabb RM, Wong PC, Wexler RR. Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2432-5. doi: 10.1016/j.bmcl.2013.02.013. Epub 2013 Feb 14. PubMed PMID: 23478148.

纯度：≥98%

CAS：1004551-40-9