Edoxaban (DU-176) 是一种选择性的，口服有效的Factor Xa (FXa)抑制剂。Edoxaban对游离FXa和凝血酶原的Ki分别为 0.561 nM 和 2.98 nM。Edoxaban 是一种抗凝剂，可用于预防中风。Edoxaban 还是一种凝血酶和凝血因子 IXaβ (FIXa) 的弱抑制剂，Ki值分别为 6.00 μM 和 41.7 μM，对FXa的选择性超过 10000 倍。由于具有抗血栓形成的特性，Edoxaban可用于预防血栓栓塞性疾病的研究。

Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with K i s of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and is able to be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with K i s of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and is potential for thromboembolic diseases treatment [1] [2] [3].

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 [1]. 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 way, 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) (IC 50 : 2.90 μM), reflecting its weak anti-thrombin activity [1]. Edoxaban is minimally metabolized (,4%) by the cytochrome P450 system (CYP3A4) and is a substrate for P-glycoprotein [2].

Edoxaban (DU-176b; 0.5-12.5 mg/kg; oral administration; Wistar rats) inhibits thrombus formation in rat thrombosis models in a dose-dependent manner [1]. Animal Model: Wistar rats (210-240 g) with venous stasis thrombosis model [1] Dosage: 0.5 mg/kg, 2.5 mg/kg, 12.5 mg/kg Administration: Oral administration Result: Dose-dependently inhibited thrombus formation in rat thrombosis models.

480449-70-5

C24H30ClN7O4S

548.06

Lixiana;依杜沙班

DMSO:130 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years