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Edoxaban

CAS No. : 480449-70-5

MCE 站：Edoxaban

产品活性：Edoxaban (DU-176) 是一种选择性，有效和口服活性的 factor Xa (FXa) 抑制剂，对游离 FXa 和凝血酶原的 K_i 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，K_i 值分别为 6.00 μM 和 41.7 μM，对 FXa 的选择性超过 10000 倍。Edoxaban 具有抗血栓形成的特性，可用于血栓栓塞性疾病的研究。

研究领域：Metabolic Enzyme/Protease

作用靶点：Factor Xa  |  Thrombin

In Vitro: 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.

In Vivo: 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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