PPAR Agonist IX, GQ-16

A cell-permeable thiazolidinedione that acts as a PPARγ-selective agonist (K_i = 160 nM) and blocks Cdk-5-mediated Ser²⁷³ phosphorylation by stabilizing PPARγ β-sheet structure, exhibiting no detectable activity towards PPARα, PPARδ, or RXRα. Although a weaker PPAPγ agonist than Thiazolidinediones (TZDs) family rosiglitazone (Cat. No. 557366; Max. fold of transactivation induction = 8.57 and 24.8 with 10 µM respective compound in U-937 reporter assays), GQ-16 can be safely administered at a higher dosage (20 mg/kg/day; oral gavage) in mice to achieve similar in vivo efficacy as rosiglitazone (4 mg/kg/day; o.g.) in reversing high fat diet-induced insulin signaling defects without adverse side effects commonly seen with TZDs.such as edema and weight gain commonly seen with TZDs.

Cell permeable: yes

Primary Target
PPARγ

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Amato, A.A., et al. 2012. J. Biol. Chem.287, 28169.

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

Toxicity: Harmful (C)