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CAS No. : 365462-23-3
MCE 国际站:Darexaban
产品活性:Darexaban (YM150) 是一种有效、选择性和具有口服活性的 Xa 因子 (FXa) 抑制剂,IC50 为 54.6 nM。Darexaban 对其他相关丝氨酸蛋白酶(如胰蛋白酶、凝血酶和激肽释放酶)显示出高选择性。Darexaban 具有抗凝和抗血栓形成作用。
研究领域:Metabolic Enzyme/Protease
作用靶点:Factor Xa | Ser/Thr Protease
In Vitro: Darexaban is an oral direct factor Xa (FXa) inhibitor that is rapidly and extensively metabolized into its glucuronide conjugate (YM-222714) post-administration. Darexaban competitively and selectively inhibits human FXa, and also inhibits the prothrombin activation induced by prothrombinase complex or whole blood clot with similar potency to free FXa.
In Vivo: In mice, Darexaban inhibits FXa activity in plasma with an ED50 value of 24.8 mg/kg. Darexaban prolonges prothrombin time (PT) at 3 mg/kg.
In a pulmonary thromboembolism (PE) mouse model, Darexaban dose-dependently reduces the mortality rate, significantly so at 10 mg/kg.
In a FeCl3-induced venous thrombosis (VT) mouse model, Darexaban (0.3-10 mg/kg) dose-dependently decreases the thrombus protein content, significantly so at doses of 3 mg/kg or higher.
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货号: HY-14853
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