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Description: Dabigatran (also known as BIBR 953 and BIBR 953ZW) is a potent, nonpeptide, reversible, selective and direct thrombin inhibitor with an IC50 of 9.3 nM in a cell-free assay. Dabigatran is designed to be converted into an orally active prodrug BIBR 1048 due to its highly polar, zwitterionic nature and poor oral absorption. Dabigatran inhibits thrombin in a competitive fashion. This inhibition is rapid and reversible. Dabigatran inhibits both clot-bound and free thrombin. Dabigatran is demonstrated to have an anticoagulant efficacy both in vitro and ex vivo.
References: J Med Chem. 2002 Apr 25;45(9):1757-66.
Related CAS#: 211915-06-9 (Dabigatran etexilate); 872728-81-9 (Dabiga tran etexilate mesylate); 211914-50-0 (Dabigatran ethyl ester HCl); 429658-95-7 (Dabigatran ethyl ester); 212321-78-3 (BIBR 1087 SE, an intermediate metabolite of dabigatran etexilate)
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: 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.
Purity ≥98%
COA
MSDS