PAR4 antagonist 9
PAR4 antagonist 9 is an orally active protease-activated receptor 4 (PAR4) antagonist with an IC50 of 2 nM against human targets. PAR4 antagonist 9 functionally modulates PAR4 and inhibits platelet aggregation. PAR4 antagonist 9 can be used in studies related to arterial thrombosis.
For research use only. We do not sell to patients.
- CAS No.: 2173066-25-4
- Formula: C29H29FN6O5S
- Molecular Weight:592.64
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PAR4 2 nM (IC50) |
In Vitro
PAR4 antagonist 9 (Compound 32) exhibits favorable metabolic stability, with a remaining ratio of 85% in the human-derived system and 100% in the rat-derived system in metabolic stability tests[1].
PAR4 antagonist 9 exhibits potent PAR4 antagonistic activity, with an FLIPR IC50 of 2 nM and a γ-Thr PRP IC50 of 4 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Cynomolgus monkeys (2 animals, healthy)[1]
-
Dosage:3 mg/kg
-
Administration:p.o.; single dose
-
Result:Achieved complete suppression of PAR4 agonist peptide-stimulated platelet aggregation at 3 h and 7 h post-dosing.
Attained plasma levels of 78.63 nM (monkey 1) and 77.87 nM (monkey 2) at 3 h, followed by concentrations of 49.44 nM (monkey 1) and 59.11 nM (monkey 2) at 7 h.
Lost sustained antithrombotic activity at 30 h post-dosing as efficacy returned to baseline, with plasma concentrations declining to 6.65 nM (monkey 1) and 1.04 nM (monkey 2).
Chemical Information
-
CAS No. 2173066-25-4
-
Molecular Weight 592.64
-
Formula C29H29FN6O5S
-
SMILES
CCOC1=NC2=CC(C)=CC(C3=NC4=C(S3)C=C(C(F)=C4)O[C@H]([C@H](OC(NC5=CN=C(N=C5)CCO)=O)C)C)=C2N=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PAR4 antagonist 9 Related Classifications
HY-183983 Related Classifications
Powered by Bioz