SR 2595

- Overview
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    Background
    
    IC50: 30 nMSR 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.
- Properties
  - Categories
    
    inverse agonist of PPARγ
    
    Alternative Name
    
    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
    
    CAS Number
    
    1415252-61-7
    
    Molecular Formula
    
    C37H38N2O3
    
    Molecular Weight
    
    558.7
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤5mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC(N1CC2=CC=C(C3=CC=CC=C3C(O)=O)C=C2)=C(C)C4=C1C=CC(C(N[[email protected]@H](C)C5=CC=C(C(C)(C)C)C=C5)=O)=C4
    
    * For Research Use Only

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

SR 2595

Background

Documents

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