product name Dabigatran (BIBR 953)
Description: 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. 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.
471.51
Formula
C25H25N7O3
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:
Ethanol: < 1 mg/mL
Solubility (In vivo)
10% Trifluoroacetic acid water solution: 33 mg/mL
Synonyms
other peoduct :
| 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2002 Apr 25;45(9):1757-66. |
