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Art. -Nr.: HY-183983

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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. Nr.: 2173066-25-4
Formel: C₂₉H₂₉FN₆O₅S
Molecular Weight:592.64

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Please store the product under the recommended conditions in the Certificate of Analysis.

PAR4 antagonist 9 Chemical Structure

CAS. Nr.: 2173066-25-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PAR4

2 nM (IC₅₀)

Alle Protease Activated Receptor (PAR) Isoform-spezifische Produkte anzeigen :

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

PAR4 antagonist 9 (Compound 32) (3 mg/kg; p.o.; single dose) produces complete, concentration-dependent inhibition of PAR4-mediated platelet aggregation for at least 7 h in cynomolgus monkeys, with effects reversing as plasma concentrations fall below 10 nM^[1].

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. Nr. 2173066-25-4
Molecular Weight 592.64
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Halpern OS, et al. Solubility-Driven Lead Optimization of PAR4 Antagonists and Evaluation of a Phosphate Ester Prodrug Delivery Strategy. ACS Med Chem Lett. 2026 May 11.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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PAR4 antagonist 9

Alle Protease Activated Receptor (PAR) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PAR4 antagonist 9 Related Classifications

HY-183983 Related Classifications