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SR 2595

Catalog No.
C5572
inverse agonist of PPARγ
Grouped product items
SizePriceStock Qty
1mg
$90.00
Ship with 5-10 days
5mg
$406.00
Ship with 5-10 days
10mg
$720.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt558.7
Cas No.1415252-61-7
FormulaC37H38N2O3
Solubility≤5mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide
Chemical Name4'-[[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
SDFDownload SDF
Canonical SMILESCC(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
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while.

Quality Control

Quality Control & MSDS

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Chemical structure

SR 2595