BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate.

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

BIBR 953; BIBR 953ZW; BIBR953; BIB-953

Powder

10% Trifluoroacetic acid water solution 33 mg/mL (69.98 mM)

DMSO 0.5 mg/mL (1.06 mM)

Ethanol 0.01 mg/mL (0.02 mM)

Thrombin

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. BIBR 953 specifically and reversibly inhibits thrombin.

BIBR 953 exhibits the most favorable activity profile following i.v. administration to rats. 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.