Edoxaban

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Edoxaban

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

480449-70-5

依度沙班
DU-176

Edoxaban (DU-176b) 是一种具有口服活性、高效、选择性和直接的Factor Xa (FXa)抑制剂，对人游离 FXa 和凝血酶原酶的K_i值分别为 0.561 nM 和 2.98 nM。Edoxaban 的选择性是其他凝血蛋白酶的 10000 倍以上。Edoxaban 可用于预防血栓栓塞性疾病的研究。

生物活性

Edoxaban (DU-176b) is an orally active, highly potent, selective, and directFactor Xa(FXa)inhibitor withK_ivalues of 0.561 and 2.98 nM for free humanFXaandprothrombinase. Edoxaban exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban can be used in preventing thromboembolic disease research^[1].

IC₅₀& Target

IC50: 2.90 μM (platelet aggregation), Ki: 0.561 nM (free human FXa), 2.98 nM (prothrombinase), 0.715 nM (cynomolgus monkey FXa), 0.457 nM (rabbit FXa)^[1]

体外研究
(In Vitro)

Edoxaban (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner^[1].
Edoxaban inhibits thrombin-induced platelet aggregation, with an IC₅₀of 2.90 μM^[1].

Cell Viability Assay^[1]

Cell Line:	Human, rat, cynomolgus monkey and rabbit plasma; Human platelet
Concentration:
Incubation Time:	1 and 5 minutes
Result:	Antithrombin.

体内研究
(In Vivo)

Edoxaban (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT^[1].

Animal Model:	Male Slc: Wistar rats (210-240 g); Male New Zealand White rabbits(2.5-3.5 kg) (Both are venous stasis thrombosis model)^[1].
Dosage:	0.5, 2.5 and 12.5 mg/kg
Administration:	Oral administration; once
Result:	Inhibited exogenous FXa activity. Antithrombotic.

Clinical Trial

分子量

548.06

性状

Solid

Formula

C₂₄H₃₀ClN₇O₄S

CAS 号

480449-70-5

中文名称

依度沙班；伊多塞班；艾多沙班

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 10 mg/mL(18.25 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.8246 mL	9.1231 mL	18.2462 mL
5 mM	0.3649 mL	1.8246 mL	3.6492 mL
10 mM	0.1825 mL	0.9123 mL	1.8246 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。