Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).
体外研究
Dabigatran (BIBR 953) shows concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human platelet-poor plasma at concentrations of 0.23, 0.83 and 0.18 μM, respectively.
体内研究
Dabigatran (0.01-0.1 mg/kg; i.v.) inhibits clot formation with an ED50 of 0.033 mg/kg in Wessler model.
Animal Model:
Male rats (Wessler model)
Dosage:
0.01, 0.03, 0.05 and 0.1 mg/kg
Administration:
Intravenous injection
Result:
Inhibited clot formation with an ED50 of 0.033 mg/kg.
分子式
C25H25N7O3
分子量
471.51
CAS号
211914-51-1
中文名称
达比加群
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:
0.1 M HCL : 12.5 mg/mL (26.51 mM; Need ultrasonic)