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货号:A112634 同义名: BIBR 953;BIBR 953ZW Ambeed 开学季,买赠积分,赢豪礼

Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.

Dabigatran 化学结构 CAS号:211914-51-1
Dabigatran 化学结构
CAS号:211914-51-1
Dabigatran 3D分子结构
CAS号:211914-51-1
Dabigatran 化学结构 CAS号:211914-51-1
Dabigatran 3D分子结构 CAS号:211914-51-1
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Dabigatran 纯度/质量文件 产品仅供科研

货号:A112634 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Thrombin 其他靶点 纯度
Dabigatran +++

Thrombin, IC50: 9.3 nM

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Dabigatran etexilate {[allProObj[0].p_purity_real_show]}
Argatroban {[allProObj[0].p_purity_real_show]}
Heparin sodium salt {[allProObj[0].p_purity_real_show]}
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。

Dabigatran 生物活性

靶点
  • Thrombin

    Thrombin, IC50:9.3 nM

描述 Dabigatran, also known as BIBR 953, is an oral anticoagulant that acts as a reversible, potent, and competitive direct thrombin inhibitor with a Ki of 4.5 nM. It also inhibits thrombin-induced platelet aggregation with an IC50 of 10 nM[1][2]. In vitro, Dabigatran exhibits concentration-dependent anticoagulant effects across different species. At a concentration of 0.23 μM, it doubles the activated partial thromboplastin time (aPTT), prothrombin time (PT), and ecarin clotting time (ECT) in human platelet-poor plasma, with respective values of 0.83 and 0.18 μM[1].

Dabigatran 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
HEK293 cells Function assay 3 mins Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50=4.7 μM 23241029

Dabigatran 动物研究

Animal study Administered intravenously at doses ranging from 0.01 to 0.1 mg/kg, Dabigatran inhibits thrombus formation in the Wessler model, with an ED50 of 0.033 mg/kg[3].

Dabigatran 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
NCT02913326 Thromboembolism Phase 3 Completed - -
NCT02171598 Healthy Phase 1 Completed - -
NCT02240654 - Completed - -

Dabigatran 参考文献

[1]Wienen W, Stassen JM, Priepke H, In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally activeprodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62.

[2]Hauel NH, et al. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66.

[3]Wienen W, et al. Effects of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate, on thrombus formation and bleeding time in rats. Thromb Haemost. 2007 Aug;98(2):333-8.

Dabigatran 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.60mL

2.12mL

1.06mL

21.21mL

4.24mL

2.12mL

Dabigatran 技术信息

CAS号211914-51-1
分子式C25H25N7O3
分子量 471.511
别名 BIBR 953;BIBR 953ZW
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

0.1 M HCL: 10 mg/mL(21.21 mM),配合低频超声助溶

动物实验配方
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