2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. 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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PAR4 antagonist 9

PAR4 antagonist 9 Chemical Structure

CAS No. : 2173066-25-4

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PAR4 antagonist 9 Related Antibodies

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Description

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[1].

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.

PAR4 antagonist 9 Related Antibodies
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).
Molecular Weight

592.64

Formula

C29H29FN6O5S
CAS No.
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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References
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PAR4 antagonist 9 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PAR4 antagonist 92173066-25-4Protease Activated Receptor (PAR)Thrombin receptorsrat liver microsomesratshuman platelet-rich plasmahuman liver microsomescynomolgus monkeysplatelet aggregationarterial thrombosisγ-thrombinProtease-activated receptor-4Inhibitorinhibitorinhibit

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