Edoxaban (DU-176b) tosylate is an highly potent, selective, and direct Factor Xa (FXa) inhibitor with K i s of 0.561 and 2.98 nM for free human FXa and prothrombinase . Edoxaban tosylate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban tosylate can be used for preventing thromboembolic disease research
In Vitro
Edoxaban tosylate (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner. Edoxaban tosylate inhibits thrombin-induced platelet aggregation, with an IC 50 of 2.90 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human, rat, cynomolgus monkey and rabbit plasma; Human platelet Concentration: Incubation Time: 1 and 5 minutes Result: Antithrombin.
In Vivo
Edoxaban tosylate (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Slc: Wistar rats (210-240 g); Male New Zealand White rabbits(2.5-3.5 kg) (Both are venous stasis thrombosis model) . Dosage: 0.5, 2.5 and 12.5 mg/kg Administration: Oral administration; once Result: Inhibited exogenous FXa activity. Antithrombotic.
Form:Solid
IC50& Target:IC50: 2.90 µM (platelet aggregation), Ki: 0.561 nM (free human FXa), 2.98 nM (prothrombinase), 0.715 nM (cynomolgus monkey FXa), 0.457 nM (rabbit FXa)
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