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AZ3451
产品别名
2100284-59-9
AZ3451
2-(6-Bromo-1,3-benzodioxol-5-yl)-N-(4-cyanophenyl)-1-[(1S)-1-cyclohexylethyl]-1H-benzimidazole-5-carboxamide
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C30H27BrN4O3 |
| Molecular weight | 571.46 |
| NACRES | NA.77 |
| Application【应用】 | AZ3451 has been used as a protease-activated receptor 2 (PAR-2) antagonist to study the involvement of PAR-2 receptors in factor X activated (FXa)-induced upregulation of the cell adhesion molecules. |
| Biochem/physiol Actions【生化/生理作用】 | AZ3451 is a potent and selective allosteric antagonist of protease-activated receptor 2 (PAR2), a G protein-coupled receptor thought to be involved in inflammatory diseases, pain, allergic associated diseases (eosinophil migration, mast cells) and cancers. AZ3451 was found to bind to a remote allosteric site outside the helical bundle that is different from the site previously found on PAR1, and had an IC50 value of 23 nM. AZ3451 was able to completely inhibit ERK phosphorylation when added to 1321N1 cells overexpressing wild-type human PAR2. AZ3451 exhibits anti-inflammatory function in vivo. It can be used as a potential therapeutic for osteoarthritis (OA). |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | N#CC1=CC=C(NC(C2=CC=C(N([C@H](C3CCCCC3)C)C(C4=CC(OCO5)=C5C=C4Br)=N6)C6=C2)=O)C=C1 |
安全信息
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
