155204-81-2

After i.v. injection to rabbits, DX-9065a displays prolonged anti-factor Xa activity and inhibition of thrombin generation^[1].
After p.o. administration, DX-9065a causes a reduction in tissue factor-induced mortality of mice with ED₅₀ value of 56 mg/kg^[1].
When given i.v. to rats, DX-9065a exhibits a dose-dependent antithrombotic effect against factor Xa + stasis-induced venous thrombosis (ED₅₀ = 1.2 mg/kg i.v.), but also in an arteriovenous shunt thrombosis model (ED₅₀ = 8.1 mg/kg i.v.) without affecting bleeding time significantly. Similar effects were obtained after s.c. or p.o. administration^[1].
In rabbits, after i.v., s.c. or p.o. administration, DX-9065a inhibits stasis-induced thrombosis after injection of tissue factor with ED₅₀ values of 0.03 mg/kg, 0.3 mg/kg and 50.5 mg/kg, respectively. DX-9065a inhibits in a dose-dependent manner endotoxin-induced venous thrombosis in the rabbit (ED₅₀ = 0.25 mg/kg i.v.) and reduces the decrease in platelet number and circulating fibrinogen levels in an experimental model of tissue factor-induced disseminated intravascular coagulation^[1].