1. Metabolic Enzyme/Protease
  2. Factor Xa
    Thrombin
  3. Edoxaban

Edoxaban (Synonyms: 依度沙班; DU-176)

目录号: HY-10264 纯度: 99.59%
产品使用指南

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 Ki 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。

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Edoxaban Chemical Structure

Edoxaban Chemical Structure

CAS No. : 480449-70-5

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Other Forms of Edoxaban:

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Edoxaban (DU-176b) is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. 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 IC50 of 2.90 µM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C24H30ClN7O4S

CAS 号
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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