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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 |
|---|
| Melagatran
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. |
| Idraparinux sodium
Idraparinux sodium (SANORG 34006) is a long-acting indirect factor Xa inhibitor. |
| Desirudin
Desirudin is a thrombin inhibitor that inhibits thrombosis and venous stasis thrombosis.Desirudin can be used in studies related to thrombocytopenia or platelet dysfunction. |
| TP508
TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. |
| Succinyl-(Pro58, D-Glu65)-Hirudin (56-65) (sulfated)
Succinyl-(Pro58,D-Glu65)-Hirudin (56-65) (sulfated) is a hirugen-like peptide, and has high affnity for thrombin than Hirugen, with a KD < 100 nM. |
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