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BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate. It has shown antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action and predictable pharmacodynamic response.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | Human thrombin is dose-dependently and competitively inhibited by dabigatran (Table 2). This inhibition with a Ki of 4.5 nmol/L compares well to the Ki of melagatran (11.2 nmol/L). Real-time binding kinetics using surface plasmon resonance showed a rapid and reversible binding of dabigatran to thrombin.7 The concentration of dabigatran required tom double the in vitro coagulation time (EC2) in platelet poor plasma is species dependent and varies with the type of test (Table 3). |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | rabbit model of venous thrombosis |
| Formulation | saline |
| Dosages | a single IV administration of 5, 10, 20, and 30 mg/kg |
| Administration | i.p. |
| Molecular Weight | 471.51 |
| Formula | C25H25N7O3 |
| CAS Number | 211914-51-1 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Thrombopoietin/Thrombin Products |
|---|
| Eltrombopag
Eltrombopag is a member of the biarylhydrazone class, which is a nonpeptide agonist of the thrombopoietin receptor (TpoR). |
| Dabigatran Etexilate
Dabigatran Etexilate is the procompound of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule. |
| Argatroban Monohydrate
Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor. |
| Dabigatran etexilate mesylate
Dabigatran etexilate mesylate is a direct thrombin inhibitor. |
| Gallic acid
Gallic acid is an antiinflammatory substance found in plants and has been shown to Induce apoptosis in human lung cancer cells. |
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