DX-9065a

DX-9065a is a selective, nonpeptidic, and orally active factor Xa (FXa) inhibitor with a K_i of 41 nM for human FXa. DX-9065a has low activity against other serine proteases. DX-9065a has strong anticoagulant actions^[1][2]. In Vitro:DX-9065a inhibits proliferation of vascular smooth muscle cells in cell culture systems^[1].
DX-9065a inactivates both free and fibrin-bound FXa^[1].
DX-9065a effectively affects the clot-associated procoagulant activity^[1].
In Vivo:DX-9065a (i.v.) displays prolonged anti-factor Xa activity and inhibition of thrombin generation in rabbits^[1].
DX-9065a (p.o.) causes a reduction in tissue factor-induced mortality of mice with ED₅₀ value of 56 mg/kg^[1].
DX-9065a inhibits stasis-induced thrombosis after injection of tissue factor with ED₅₀ values of 0.03 mg/kg for i.v., 0.3 mg/kg for s.c. and 50.5 mg/kg for p.o., respectively^[1].