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首页 / 抑制剂/激动剂 / 代谢酶 / Factor Xa / Edoxaban

依度沙班 /Edoxaban {[allProObj[0].p_purity_real_show]}

货号：A587736 同义名： 依杜沙班 / DU-176;Savaysa

Edoxaban is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.

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Edoxaban 化学结构 CAS号：480449-70-5
Edoxaban 化学结构
CAS号：480449-70-5
Edoxaban 3D分子结构
CAS号：480449-70-5
Edoxaban 化学结构 CAS号：480449-70-5
Edoxaban 3D分子结构 CAS号：480449-70-5
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Edoxaban 纯度/质量文件 产品仅供科研

货号：A587736 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Factor Xa ↓ 其他靶点 纯度
Rivaroxaban ++

Factor Xa, IC50: 0.7 nM

 		98%
Apixaban ++++

Factor Xa (rabbit), Ki: 0.17 nM

Factor Xa (human), Ki: 0.08 nM

 		98%
Edoxaban tosylate monohydrate +++

Factor Xa, Ki: 0.561 nM

 		98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Edoxaban 生物活性

描述 Factor Xa (FXa) is a coagulation factor thrombokinase responsible for the generation of thrombin. Edoxaban is a direct, selective FXa inhibitor with a Ki value of 0.561nM. In uman plasma samples, the minimum concentrations of edoxaban needed to significantly prolong prothrombin time (PT) and activated partial thromboplastin time were 55 and 50ng/mL, respectively. Plasma edoxaban at the concentration of 5.5 – 1640 ng/ml inhibited the generation of thrombin in a dose-dependent manner. Edoxaban above 10 ng/ml significantly extended the initiation phase of thrombin generation. In human platelet-poor plasma, the peak IC50 value, mRate IC50 value, and endogenous thrombin potential (ETP) IC50 value measured in thrombin generation assay were 0.145, 0.047, and 1.39 µM, respectively. The doses of edoxaban required to reach 50% of inhibition of CT2 lag time and ttPeak were 0.188 and 0.139 µM, respectively. In human platelet-rich plasma, the peak IC50, mRate IC50, and ETP IC50 values were 0.305, 0.230, and 0.636 µM, respectively. In apolipoprotein E (ApoE)-deficient mice, the treatment with 15 mg/kg edoxaban one hour before vascular injury almost completely prevented thrombus formation, and significantly decreased the time to occlusion and the patency rate. The following chronic oral administration of 10 mg/kg edoxaban by gavage b.i.d for six weeks significantly suppressed neointimal hyperplasia.
作用机制 Edoxaban inhibits free FXa by directly binding to FXa without the need of antithrombin, thereby preventing the conversion of prothrombin to thrombin.

Edoxaban 动物研究

Dose Rat: 0.3 mg/kg - 3 mg/kg[3] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[4]
Dose 1 mg/kg
Administration p.o. or i.v.
AUC0→24h 212 ± 87 ng·h/ml (p.o.)
545 ± 21 ng·h/ml (i.v.)
AUC0-inf 301 ng·h/ml (p.o.)
539 ± 29 ng·h/ml (i.v.)
T1/2 4.85 ± 2.88 h (p.o.)
1.32 ± 0.69 h (i.v.)
Tmax 0.500 ± 0.000 h (p.o.)
AUClast 184 ± 94 ng·h/ml (p.o.)
516 ± 29 ng·h/ml (i.v.)
CL 1.86 ± 0.10 L/h/kg (i.v.)
Cmax 72.7 ± 35.7 ng/ml (p.o.)
Vss 2.14 ± 0.36 L/kg (i.v.)

Edoxaban 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00986154 Venous Thromboembolism ... 展开 >> Deep Vein Thrombosis (DVT) Pulmonary Embolism (PE) Thromboembolism Venous Thrombosis 收起 << Phase 3 Completed - -
NCT02219984 - Active, not recruiting July 2019 Italy ... 展开 >> S. Orsola-Malpighi University hospital Bologna, BO, Italy, 40138 收起 <<
NCT02611635 - Completed - Sweden ... 展开 >> Multiple Locations, Sweden 收起 <<

Edoxaban 参考文献

[1]Goette A, Merino JL, et al. Edoxaban versus enoxaparin-warfarin in patients undergoing cardioversion of atrial fibrillation (ENSURE-AF): a randomised, open-label, phase 3b trial. Lancet. 2016 Oct 22;388(10055):1995-2003.

[2]Bounameaux H, Camm AJ. Edoxaban: an update on the new oral direct factor Xa inhibitor. Drugs. 2014 Jul;74(11):1209-31.

[3]Morishima Y, Honda Y, et al. Prevention of Stent Thrombosis in Rats by a Direct Oral Factor Xa Inhibitor Edoxaban. Pharmacology. 2019;103(1-2):17-22.

[4]DU-176

Edoxaban 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.82mL

0.36mL

0.18mL

9.12mL

1.82mL

0.91mL

18.25mL

3.65mL

1.82mL

Edoxaban 技术信息

CAS号480449-70-5
分子式C24H30ClN7O4S
分子量 548.058
别名 依杜沙班 ;DU-176;Savaysa;DU-176b
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C
溶解度

DMSO: 9 mg/mL(16.42 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Edoxaban | 480449-70-5 | DU-176 | DU176 | DU 176 | FXa Inhibitor | Metabolic Enzyme/Protease | Factor Xa | Thrombin | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Edoxaban 纯度/质量文件 | Edoxaban 亚型比较 | Edoxaban 生物活性 | Edoxaban 动物研究 | Edoxaban 临床数据 | Edoxaban 参考文献 | Edoxaban 实验方案 | Edoxaban 技术信息

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