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      Dabigatran Etexilate
      Dabigatran Etexilate

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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 #: V1849
      CAS #: 211915-06-9Purity ≥98%

      Description: Dabigatran Etexilate (BIBR-1048) is the prodrug of dabigatran which is a potent and nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule. Dabigatran (also known as IBR 953) is a potent nonpeptide 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.

      References: J Med Chem. 2002 Apr 25;45(9):1757-66; Thromb Haemost. 2007 Jul;98(1):155-62.

      Related CAS#: 872728-81-9 (Dabigatran etexilate mesylate); 211914-51-1 (Dabigatran); 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)627.73
      FormulaC34H41N7O5
      CAS No.211915-06-9
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 126 mg/mL (200.7 mM)
      Water: <1 mg/mL
      Ethanol: 12 mg/mL (19.1 mM)
      Other info
      		Chemical Name: (E)-ethyl 3-(2-(((4-(N'-((hexyloxy)carbonyl)carbamimidoyl)phenyl)amino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoate
      InChi Key: KSGXQBZTULBEEQ-UHFFFAOYSA-N
      InChi Code: InChI=1S/C34H41N7O5/c1-4-6-7-10-21-46-34(44)39-32(35)24-12-15-26(16-13-24)37-23-30-38-27-22-25(14-17-28(27)40(30)3)33(43)41(20-18-31(42)45-5-2)29-11-8-9-19-36-29/h8-9,11-17,19,22,37H,4-7,10,18,20-21,23H2,1-3H3,(H2,35,39,44)
      SMILES Code: O=C(OCC)CCN(C1=NC=CC=C1)C(C2=CC=C3N(C)C(CNC4=CC=C(/C(N)=N\C(OCCCCCC)=O)C=C4)=NC3=C2)=O 
      SynonymsBIBR 1048; BIBR1048; BIBR-1048; BIBR 953; BIBR-953; BIBR953; Pradaxa and Prazaxa


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      In Vitro

      In vitro activity: Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran inhibits thrombin generation in platelet-poor plasma (PPP) with IC50 of 0.56 μM, measured as the endogenous thrombin potential (ETP). Dabigatran demonstrates concentrationdependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 μM, respectively.

      In VivoDabigatran prolongs the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dabigatran etexilate (20 mg/kg, orally) produces less prolongation of K value and less decreases in angle and maximum amplitude than enoxaparin in swine. Dabigatran (0.01-0.1 mg/kg) reduces thrombus formation dose-dependently, with an ED50 (50% of the effective dose) of 0.033 mg/kg and complete inhibition at 0.1 mg/kg. Dabigatran etexilate (5-30 mg/kg) inhibits thrombus formation in a dose- and time-dependent manner, with maximum inhibition within 30 min of pretreatment, suggesting a rapid onset of action.
      Animal modelRats and monkeys
      Formulation & DosageIntravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg).
      ReferencesJ Med Chem. 2002 Apr 25;45(9):1757-66; Thromb Haemost. 2007 Jul;98(1):155-62; J Thorac Cardiovasc Surg. 2011 Jun;141(6):1410-6. 

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

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