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AC-55541 {[allProObj[0].p_purity_real_show]}

货号:A129091

AC-55541是一种小分子 PAR2 激动剂,在细胞增殖、磷脂酰肌醇水解和钙离子动员测定中的效能范围为 200 至 1000 nM。

AC-55541 化学结构 CAS号:916170-19-9
AC-55541 化学结构
CAS号:916170-19-9
AC-55541 3D分子结构
CAS号:916170-19-9
AC-55541 化学结构 CAS号:916170-19-9
AC-55541 3D分子结构 CAS号:916170-19-9
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AC-55541 纯度/质量文件 产品仅供科研

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AC-55541 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].

AC-55541 参考文献

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

AC-55541 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.65mL

1.93mL

0.96mL

19.29mL

3.86mL

1.93mL

AC-55541 技术信息

CAS号916170-19-9
分子式C25H20BrN5O3
分子量 518.362
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Store in freezer, under -20°C

溶解方案

DMSO: 50 mg/mL(96.46 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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