Bivalirudin TFA is a synthetic 20 residue peptide which reversibly inhibits thrombin. IC50 Value: Target: thrombin in vitro: Eptifibatide (8 mg/mL) added together with a low (70 ng/mL) concentration of bivalirudin (a direct thrombin inhibitor) effectively (approximately 90%) reduced platelet aggregation induced by thrombin (0.2 U/mL). In thrombin generation assay (TGA), bivalirudin had no effect on these parameters up to 10 μmol/l. Bivalirudin-facilitated binding of MPO to BAEC resulted also in functional changes in terms of increased NO consumption as well as enhanced MPO-mediated redox modifications. in vivo: The use of bivalirudinprevented further increase in antiheparin/PF4 antibody IgG levels in rats. Three animals in the 500-mg/kg/24 h group, and 7 animals in the 2000-mg/kg/24 h group in the toxicokinetic assessment phase of the study were found dead or euthanized in extremis (following blood sampling). Plasma concentrations of bivalirudin appeared to be linear and dose independent. Clinical trial: Antithrombotic Effects of Ticagrelor Versus Clopidogrel . Phase 4
| Molecular Weight | 2294.34 |
| CAS Number | 1191386-55-6 |
| Solubility (25°C) | Water 90 mg/mL DMSO ≥ 31 mg/mL |
| Storage | -20°C, protect from light, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Thrombopoietin/Thrombin Products |
|---|
| 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. |
| Thrombin receptor peptide ligand
Thrombin receptor peptide ligand is a thrombin receptor antagonist peptide that can be used as an antithrombotic agent. |
| Z-Gly-Pro-Arg-4MβNA
Z-Gly-Pro-Arg-4MβNA is the cleavage of the substrate of thrombin to release free 4-methoxy-2-naphthylamine (4MβNA). |
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