Molecular Formula | C29H33FN2O4 |
Molar Mass | 492.58 |
Density | 1.24±0.1 g/cm3(Predicted) |
Boling Point | 676.0±55.0 °C(Predicted) |
Flash Point | 362.632°C |
Vapor Presure | 0mmHg at 25°C |
pKa | 12.49±0.60(Predicted) |
Storage Condition | 2-8℃ |
Refractive Index | 1.594 |
In vitro study | SCH530348, a synthetic tricyclo-3-phenylpyridine, is an orally effective Thrombin Receptor Antagonist. SCH530348 effectively inhibited thrombin-induced platelet aggregation, IC5047 nM, and also effectively inhibited haTRAP-induced platelet aggregation, IC50 25 nM, but did not inhibit other agonists such as ADP, platelet aggregation induced by collagen and PAR-4 agonist peptides. SCH530348 had no effect on prothrombin time (PT), partial thromboplastin time (PTT), or activated partial thromboplastin time (aPTT). Moreover, SCH530348 did not cause an increase in bleeding time or surgical bleeding compared to the inactive control group. SCH530348 acts on several ion channels and receptors, including the PAR-4 receptor, while selectively acting on PAR-1. |
In vivo study | The SCH 530348 was absorbed by 68% and 82% in rats and monkeys treated with 10 mg/kg and 1 mg/kg, respectively. Treated rats and monkeys had T max of 3 and 1 hour, elimination half-lives of 5.1 and 13 hours, and oral bioavailability of 33% and 86%, respectively. In a preclinical study, SCH 530348 inhibited 100% thrombin receptor agonist peptide (TRAP)-induced platelet aggregation by oral treatment of cynomolgus monkey platelets at a dose of more than 0.1 mg/kg, inhibition was up to 24 hours, with partial recovery occurring at 48 hours. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.03 ml | 10.151 ml | 20.301 ml |
5 mM | 0.406 ml | 2.03 ml | 4.06 ml |
10 mM | 0.203 ml | 1.015 ml | 2.03 ml |
5 mM | 0.041 ml | 0.203 ml | 0.406 ml |