4′-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]- [1,1′-Biphenyl]-2-carboxylic acid

产品名称：

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

产品介绍：

产品说明

包装

5, 25 mg in glass bottle

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.

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.

其他说明

Light sensitive

基本信息

经验(实验)分子式	C₃₃H₂₉N₃O₅
分子量	547.60
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
储存条件	protect from light
颜色	white to beige
溶解性	DMSO: 15 mg/mL, clear
储存温度	−20℃

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable