KKL 顾客使用本产品发表的 1 篇科研文献

Edoxaban tosylate (DU-176b) is a selective, potent and orally active factor Xa (FXa) inhibitor with K_is of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban tosylate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with K_is of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate has antithrombotic properties and has potential for thromboembolic diseases treatment.

Edoxaban (DU-176b) also inhibits rat, cynomolgus monkey and rabbit FXa with K_i values of 6.90 nM, 0.715 nM and 0.457 nM, respectively.
Prothrombin time (PT), activated partial thromboplastin time (APTT) and thrombin time (TT) of human plasma are prolonged by Edoxaban (DU-176b) in a concentration-dependent manner, doubling PT and APTT at 0.256 and 0.508 μM, respectively. The double clotting time (CT2) for TT, however, was much higher (4.95 μM), reflecting its anti-thrombin activity. Thrombin-induced platelet aggregation is inhibited by a high concentration of Edoxaban (DU-176b) (IC₅₀: 2.90 μM), reflecting its weak anti-thrombin activity.
Edoxaban is minimally metabolized (,4%) by the cytochrome P450 system (CYP3A4) and is a substrate for P-glycoprotein.

Edoxaban (DU-176b; 0.5-12.5 mg/kg; oral administration; Wistar rats) dose-dependently inhibits thrombus formation in rat thrombosis models.

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