516570-M

PPARγ Modulator, SR1664

A cell-permeable non-thiazolidinediones derivative that binds tightly to peroxisome proliferator-activated γ (PPAR-γ) receptor, but does not exhibit any transcriptional agonism.

• Synonym(s): PPARγ Modulator, SR1664, (S)-4′-((2,3-dimethyl-5-(1-(4-nitrophenyl)ethylcarbamoyl)-1H-indol-1-yl)methyl)biphenyl-2-carboxylic acid
• Empirical Formula (Hill Notation): C₃₃H₂₉N₃O₅
• Molecular Weight: 547.60
• UNSPSC Code: 12352200

Properties

• assay: ≥92% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: red
• solubility: DMSO: 50 mg/mL
• storage temp.: −20°C

Description

General description

A cell-permeable non-thiazolidinediones derivative that binds tightly to peroxisome proliferator-activated γ (PPAR-γ) receptor (K_i = 29 nM; IC₅₀ = 80 nM), but does not exhibit any transcriptional agonism. Unlike TZD compounds, it does not induce weight gain or diminish hematocrit. Shown to effectively block CDK-5-mediated phosphorylation of Ser²⁷³ of PPAR-gamma in adipose tissue. Supresses hepatic glucose production, reduces plasma free fatty acid levels, and improves insulin sensitivity of adipose tissue.

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Choi, J., et al. 2011, Nature477, 477.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable