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CAS No.: 916170-19-9

AC-55541 Catalog No. CSN18572

Synonyms: N/A

AC-55541 is a small-molecule protease-activated receptor 2 (PAR2) agonist and activates PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Protease activated receptors (PARs) are a family of four G-protein-coupled receptors (PAR1, PAR2, PAR3, and PAR4) that are self-activated by tethered peptide ligands exposed by proteolytic cleavage of the extracellular amino terminus. PAR2 receptors have been implicated in numerous physiological processes necessitating therapeutic intervention, especially pain and inflammation and syndromes with a strong inflammatory component, including colitis, gastritis, pancreatitis, asthma and pulmonary disease. AC-55541 is a highly selective PAR2 agonist with pEC₅₀ value of 6.7. Concentration-response experiments demonstrated that AC-55541 stimulated cellular proliferation in a PAR2-specific manner. The potencies of AC-55541 in the cellular proliferation assay was approximately 200 nM at the protease-insensitive mutant PAR2 S37P , and was virtually the same at wild-type PAR2 receptors. In the PI hydrolysis assays, AC-55541 had potency of approximately 1 to 3M. In the Ca²⁺ mobilization assay, AC-55541 had potency of approximately 250 nM. Intraperitoneal administration of AC-55541 resulted in peak plasma concentration of 1035 ng/ml at 50 min in male Sprague-Dawley rats. The elimination half-live of AC-55541 was 6.1 h. AC-55541 was reasonably stable to metabolism in the presence of liver microsomes, with values of 6 and 19 μL/min/mg for AC-55541 in human and rat liver microsomes, respectively. Moreover, intrapaw administration of AC-55541 resulted in hind paw edema and thermal hyperalgesia at doses as low as 30 ng^[1].
参考文献

[1] Identification and characterization of novel small-molecule protease-activated receptor 2 agonists

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9292 mL
- 9.6458 mL
- 19.2915 mL
- 5 mM
- 0.3858 mL
- 1.9292 mL
- 3.8583 mL
- 10 mM
- 0.1929 mL
- 0.9646 mL
- 1.9292 mL

技术信息

CAS号

916170-19-9

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H20BrN5O3

运输

蓝冰

分子量

518.36

别名

N/A

溶解度

DMSO	7.0 mg/mL (13.5 mM) warming
Water	insoluble

动物实验配方

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AC-55541 Catalog No. CSN18572

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