1478711-48-6
1478711-48-6 structure
- Name: BMS-986141
- Chemical Name: BMS-986141
- CAS Number: 1478711-48-6
- Molecular Formula: C27H23N5O5S2
- Molecular Weight: 561.63
- Catalog: Signaling Pathways GPCR/G Protein Protease-Activated Receptor (PAR)
- Create Date: 2022-09-12 12:05:07
- Modify Date: 2024-04-05 19:50:07
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BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect[1][2].
| Name | BMS-986141 |
|---|
| Description | BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect[1][2]. |
|---|---|
| Related Catalog | |
| Target |
PAR4:0.4 nM (IC50) |
| In Vitro | BMS-986141 (compound 49) (0-1 μM) inhibits platelet aggregation induced by PAR4 agonist peptide with an IC50 value of 2.2 nM[1]. |
| In Vivo | BMS-986141 (compound 49) shows a slight but significant prolongation of KBT (kidney bleeding time) and demonstrates excellent anti-thrombotic efficacy at 0.5 mg/kg in cynomolgus monkey[1][2]. Animal Model: Monkey arterial thrombosis (AT) and mesenteric bleeding time (MBT) models[2] Dosage: 0.05, 0.1, 0.5 mg/kg Administration: p.o., 2 hours Result: Inhibited PAR4-AP-induced platelet aggregation in human and monkey blood with IC50 of 1.8 and 1.3 nM, respectively. Reduced the thrombus weight by 36%, 63% and 88% at concentrations of 0.05, 0.1 and 0.5 mg/kg, respectively in AT model. Increased MBT by 1.2 times. Animal Model: Rat, dog and monkey[1] Dosage: 0.5, 1, 2 mpk Administration: i.v., 0.5 mpk, 10 min or p.o., 2 mpk for rat, 1 mpk for dog and monkey Result: The pharmacokinetic parameters of BMS-986141 (compound 49) Parameters rat dog monkey t1/2(h) 3.7 ± 0.4 13 75 ± 12 CL (mL/min/kg) 14.3 ± 0.4 8.5 12 ± 2 Vss(L/kg) 2.7 ± 0.3 2.7 14 ± 5 F (%) 31 25 36 |
| References |
| Molecular Formula | C27H23N5O5S2 |
|---|---|
| Molecular Weight | 561.63 |