Edoxaban (hydrochloride)

Edoxaban (DU-176b) hydrochloride is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with K_i values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban hydrochloride exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban hydrochloride can be used for preventing thromboembolic disease research^[1]. 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)^[1] In Vitro: Edoxaban hydrochloride (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner^[1].
Edoxaban hydrochloride inhibits thrombin-induced platelet aggregation, with an IC₅₀ of 2.90 µM^[1]. In Vivo: Edoxaban hydrochloride (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT^[1].