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.
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- CAS No.: 2173066-25-4
- Formule: C29H29FN6O5S
- Masse moléculaire:592.64
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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PAR4 2 nM (IC50) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkeys (2 animals, healthy)[1]
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Dosage:3 mg/kg
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Administration:p.o.; single dose
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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
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CAS No. 2173066-25-4
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Masse moléculaire 592.64
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Formule C29H29FN6O5S
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PAR4 antagonist 9 Related Classifications
HY-183983 Related Classifications
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