SR 2595

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

Product information

CAS Number: 1415252-61-7

Molecular Weight: 558.71

Formula: C37H38N2O3

Chemical Name: 4'-[(5-{[(1S)-1-(4-tert-butylphenyl)ethyl]carbamoyl}-2,3-dimethyl-1H-indol-1-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid

Smiles: C[C@H](NC(=O)C1=CC2=C(C=C1)N(CC1C=CC(=CC=1)C1=CC=CC=C1C(O)=O)C(C)=C2C)C1C=CC(=CC=1)C(C)(C)C

InChiKey: WKDKAVKAQXVFJV-DEOSSOPVSA-N

InChi: InChI=1S/C37H38N2O3/c1-23-25(3)39(22-26-11-13-28(14-12-26)31-9-7-8-10-32(31)36(41)42)34-20-17-29(21-33(23)34)35(40)38-24(2)27-15-18-30(19-16-27)37(4,5)6/h7-21,24H,22H2,1-6H3,(H,38,40)(H,41,42)/t24-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

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