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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 2173066-25-4
分子式: C₂₉H₂₉FN₆O₅S
分子量:592.64

保管条件:

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

PAR4 antagonist 9 構造式

CAS 番号: 2173066-25-4

価格（税別）

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
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生物活性

製品説明

IC₅₀ & Target

^[1]

PAR4

2 nM (IC₅₀)

Protease Activated Receptor (PAR) アイソフォーム固有の製品をすべて表示 :

体外実験

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.

体内実験

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).

化学情報

CAS 番号 2173066-25-4
分子量 592.64
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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

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

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希釈計算機

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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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MOQ

Minimum order quantity

100 mg

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