Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | cynomolgus monkeys |
| Formulation | 0.4% methyl cellulose |
| Dosages | 0.5, 0.3, 0.1, and 0.05 mg/kg |
| Administration | oral |
| Molecular Weight | 492.58 |
| Formula | C29H33FN2O4 |
| CAS Number | 618385-01-6 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 PAR Products |
|---|
| TRAP-6 amide
TRAP-6 amide is a PAR-1 thrombin receptor agonist peptide. |
| Protease-Activated Receptor-1, PAR-1 Agonist
Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. |
| FSLLRY-NH2
FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor. |
| iso-TRAP-6
iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. |
| PAR-4 Agonist Peptide, amide
PAR-4 Agonist Peptide, amide (PAR-4-AP; AY-NH2) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist. |
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