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    Dabigatran (BIBR 953)
    Dabigatran (BIBR 953)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1848
    CAS #: 211914-51-1 Purity ≥98%

    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)

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    Molecular Weight (MW)471.51 
    FormulaC25H25N7O3 
    CAS No.211914-51-1 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 0.5 mg/mL (1.06 mM)  
    Water: N/A
    Ethanol: < 1 mg/mL
    Solubility (In vivo)10% Trifluoroacetic acid water solution: 33 mg/mL 
    SynonymsBIBR 953; BIBR-953; BIBR953; Dabigatran Etexilate; Pradaxa and Prazaxa


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    In Vitro

    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.

    In VivoBIBR 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. 
    Animal modelRats
    Formulation & Dosagep.o. and i.v. administration to rats
    ReferencesJ Med Chem. 2002 Apr 25;45(9):1757-66. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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