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SR1664
产品别名
1338259-05-4
SR1664
4′-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]- [1,1′-Biphenyl]-2-carboxylic acid
基本信息
| Empirical Formula【经验(实验)分子式】 | C33H29N3O5 |
| Molecular weight | 547.60 |
| NACRES | NA.77 |
| Biochem/physiol Actions【生化/生理作用】 | SR1664 is a non-agonist PPARγ ligand and an inhibitor of Cdk5-mediated PPARγ phosphorylation. It has strong antidiabetic activity in two murine models of diabetes without the side effects normally asociated with the thiazolidinedione (TZD) antidiabetic PPARγ agonists. The TZD antidiabetics such as rosiglitazone and pioglitazone are full PPARγ agonists, but recent data have suggested that their separate activity, inhibition of the the obesity-linked PPARγ phosphorylation by Cdk5, is likely the more important activity for antidiabetic action. SR1664 has an IC50 of 80 nM in a competitive binding assay, blocked the Cdk5-mediated phosphorylation of PPARγ in vitro with IC50 between 20 and 200 nM and exhibited no PPARγ agonist activity. |
| Features and Benefits【特点和优势】 | This compound is featured on the CDKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here. |
| Other Notes【其他说明】 | Light sensitive |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| storage condition【储存条件】 | protect from light |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 15 mg/mL, clear |
| storage temp.【储存温度】 | −20℃ |
| packaging【包装】 | 5, 25 mg in glass bottle |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
