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产品名称 | Thrombin ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Dabigatran |
+++
Thrombin, IC50: 9.3 nM |
98% | |||||||||||||||||
Dabigatran etexilate | ✔ | 98% | |||||||||||||||||
Argatroban | 99%+ | ||||||||||||||||||
Heparin sodium salt | ✔ | ≥150 u/mg | |||||||||||||||||
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。 |
靶点 |
|
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 |
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]. |
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 | - | - | |
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 |
CAS号 | 211914-51-1 |
分子式 | C25H25N7O3 |
分子量 | 471.51 |
SMILES Code | O=C(O)CCN(C(C1=CC=C2C(N=C(CNC3=CC=C(C(N)=N)C=C3)N2C)=C1)=O)C4=NC=CC=C4 |
MDL No. | MFCD09837830 |
别名 | BIBR 953; BIBR 953ZW |
运输 | 蓝冰 |
InChI Key | YBSJFWOBGCMAKL-UHFFFAOYSA-N |
Pubchem ID | 216210 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, room temperature |
溶解方案 |
0.1 M HCL: 10 mg/mL(21.21 mM),配合低频超声助溶 |