| Name | Bivalirudin |
| Description | Bivalirudin (BG-8967) is a reversible inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities. |
| Animal Research | Animals were randomly assigned to one of five groups: control (no aspirin or hirulog); aspirin alone (10 mg/kg); aspirin plus low-dose hirulog (0.2 mg/kg bolus followed by 0.5 mg/kg/hr); aspirin plus medium-dose hirulog (0.4 mg/kg bolus followed by 1.0 mg/kg/hr); or aspirin plus high-dose hirulog (0.6 mg/kg bolus followed by 1.5 mg/kg/hr). Hirulog was infused before surgery and continued until termination of the experiment 30 minutes after endarterectomy [3]. |
| In vitro | Whereas 0.1 microM-hirudin and 0.1 microM-Bivalirudin (i.e. less than 10% of the concentration of prothrombin in plasma) inhibited Factor X, Factor V, and prothrombin activation. Concentrations of hirudin and hirulog-1 equimolar to and 5 times greater than those of alpha-thrombin respectively abrogated Factor V activation by exogenous alpha-thrombin [2]. |
| In vivo | Deposition in aspirin-treated groups receiving low-, medium-, and high-dose Bivalirudin decreased in a dose-dependent manner by 37%, 44%, and 56%, respectively. As the dose of Bivalirudin was increased, the plasma Bivalirudin levels and activated partial thromboplastin time ratios (final: initial) also increased in a dose-dependent manner. The mean plasma Bivalirudin levels ranged from 0.74 micrograms/ml in the low-dose Bivalirudin group to 2.55 micrograms/ml in the high-dose Bivalirudin group, and the corresponding activated partial thromboplastin time ratios were 1.5 and 3.3 [3]. |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 10 mM
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| Keywords | BG8967 | anticoagulation | invasive | peptide | coronary | Inhibitor | platelets | percutaneous | Bivalirudin | anticoagulant | Thrombin | inhibit | cardiology | BG 8967 |
| Inhibitors Related | (S)-(+)-Ibuprofen | AEBSF hydrochloride | Heparin sodium salt |
| Related Compound Libraries | ReFRAME Related Library | Protease Inhibitor Library | Peptide Compound Library | NO PAINS Compound Library |
United States
