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SR 2595
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SR 2595图片
CAS NO: 1415252-61-7
包装与价格：
包装 价格(元)
1mg 电议
5mg 电议
10mg 电议

半岛bd体育手机客户端 介绍
SR 2595 是 PPARγ 的反向激动剂，IC50 为 30 nM。
Cas No. 1415252-61-7
化学名 4'-[[5-[[[(1S)-1-[4-(1,1-dimethylethyl)phenyl]ethyl]amino]carbonyl]-2,3-dimethyl-1H-indol-1-yl]methyl]-[1,1'-biphenyl]-2-carboxylic acid
Canonical SMILES CC(N1CC2=CC=C(C3=CC=CC=C3C(O)=O)C=C2)=C(C)C4=C1C=CC(C(N[C@@H](C)C5=CC=C(C(C)(C)C)C=C5)=O)=C4
分子式 C37H38N2O3
分子量 558.7
溶解度 ≤5mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide
储存条件 Store at -20℃
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

IC50: 30 nM

SR 2595 is an inverse agonist of PPARγ.

The nuclear receptor peroxisome proliferator-activated receptor gamma (PPARγ) is the key regulator of adipogenesis and the pharmacological target of the thiazolidinedione class of insulin sensitizers. Activation of PPARγ by thiazolidinediones can promote adipogenesis at the expense of osteoblast formation.

In vitro: SR 2595 was identified as an inverse agonist of PPARγ that repressed both transactivation and expression of the adipogenic marker fatty acid-binding protein 4 in differentiating murine preadipocytes. Moreover, the repression of PPARγ with SR 2595 promoted osteogenesis in cultured human mesenchymal stem cells (MSCs), as demonstrated by calcium phosphatase deposition. In addition, SR 2595 could also increase the expression of bone morphogenetic proteins BMP2 and BMP6 in MSCs [1].

In vivo: To determine whether pharmacological PPARg repression would impair insulin sensitivity, SR2595 was administered chronically to lean C57BL/6J mice. The PK properties of SR2595 were sufficient to support once daily oral dosing at 20 mg/kg. Lean C57BL/6J mice treated with SR2595 showed no significant change in insulin sensitivity as measured by insulin tolerance test, nor fasting insulin levels. In addition, no change in food consumption or body weight was observed during the treatment period [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Marciano, D. P.,Kuruvilla, D.S.,Boregowda, S.V., et al. Pharmacological repression of PPARγ promotes osteogenesis. Nature Communications 6, 1-7 (2015).
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