Dabigatran [211914-51-1]

Dabigatran (BIBR 953ZW) 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.

Thrombin:9.3 nM

Dabigatran is a very potent anticoagulant. Dabigatran shows that the terminal phenyl can be substituted by the more hydrophilic 2-pyridyl group without substantial loss of activity. Dabigatran 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] Dabigatran specifically and reversibly inhibits thrombin. [2]

Dabigatran 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]

0.1 M HCL: 12.5 mg/mL (26.51 mM), Sonication is recommended.

DMSO: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 0.1 mg/mL (insoluble)