| CAS NO: | 211914-51-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 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: N/A | |
| Ethanol: < 1 mg/mL | |
| Solubility (In vivo) | 10% Trifluoroacetic acid water solution: 33 mg/mL |
| Synonyms | BIBR 953; Pradaxa; BIBR953; BIBR-953; Dabigatran Etexilate; Prazaxa |
| 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 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 | Rats |
| Formulation & Dosage | p.o. and i.v. administration to rats |
| References | J Med Chem. 2002 Apr 25;45(9):1757-66. |
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