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抑制剂/激活剂

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凋亡与自噬

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Edoxaban 依度沙班；伊多塞班

Edoxaban (DU-176b, Savaysa) 是一种抗血栓形成剂，是一种选择性的、有效的 factor Xa (FXa) 口服抑制剂，其对游离的FXa和促凝血球蛋白的Ki值分别为0.561 nM和2.98 nM。

货号：
TK0565
规格：

1mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	480449-70-5
生物活性	Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment.
分子式	C24H30ClN7O4S
分子量	548.06
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder, -20°C ,3 years
溶解性数据	DMSO : 10 mg/mL (18.25 mM; Need ultrasonic)
体内研究	Edoxaban (DU-176b; 0.5-12.5 mg/kg; oral administration; Wistar rats) dose-dependently inhibits thrombus formation in rat thrombosis models.
体外研究	Edoxaban (DU-176b) also inhibits rat, cynomolgus monkey and rabbit FXa with Ki 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.
纯度及产品资料	98%

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