Dabigatran

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Chemical Structure| 211914-51-1 同义名 : BIBR 953; BIBR 953ZW
CAS号 : 211914-51-1
货号 : A112634
分子式 : C25H25N7O3
纯度 : 98%
分子量 : 471.51
MDL号 : MFCD09837830
存储条件：

Pure form Keep in dark place, inert atmosphere, room temperature

In solvent -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
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].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 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
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 - -
实验方案
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
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.