Biochem/physiol Actions

Reversible: yes

Primary TargetPPARγ

Cell permeable: yes

General description

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.

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.) without adverse side effects commonly seen with TZDs.

Legal Information

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

Other Notes

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

Packaging

25 mg in Glass bottle

Packaged under inert gas

Reconstitution

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

Warning

Toxicity: Harmful (C)