Dabigatran 是一种口服抗凝剂，是一种可逆的，竞争性的直接凝血酶 (Thrombin) 抑制剂，Ki=4.5 nM。它也抑制凝血酶诱导的血小板聚集 (IC50=10 nM)。

Dabigatran is a THROMBIN inhibitor which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation. It is used to reduce the risk of stroke and systemic EMBOLISM in patients with nonvalvular atrial fibrillation.

BIBR 953 is a very potent anticoagulant. BIBR 953 shows that the terminal phenyl can be substituted by the more hydrophilic 2-pyridyl group without substantial loss of activity. BIBR 953 inhibits thrombin, plasmin, factor Xa, trypsin, tPA and activated protein C with Ki of 4.5 nM, 1.7 μM, 3.8 μM, 50 nM, 45 μM and 20 μM, respectively. [1] BIBR 953 specifically and reversibly inhibits thrombin. [2]

BIBR 953 exhibits the most favorable activity profile following i.v. administration to rats. [1] The bioavailability of dabigatran after p.o. administration of dabigatran etexilate is 7.2%. Dabigatran is predominantly excreted in the feces after p.o. treatment and in the urine after i.v. treatment. The mean terminal half-life of dabigatran is approximately 8 hours. Dabigatran acylglucuronides accounts for 0.4% and 4% of the dose in urine after p.o. and i.v. dosing, respectively. [3]

211914-51-1

C25H25N7O3

471.51

达比加群;BIBR 953;BIBR 953ZW

0.1 M HCL:12.5 mg/mL (26.51 mM),Need ultrasonic
DMSO:< 1 mg/mL (insoluble or slightly soluble)
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years