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GQ-16 is a novel partial agonist of peroxisome proliferator-activated receptor γ (PPARγ) involved in promoting insulin sensitization [1]. PPAR-γ is mainly involved in fat cell differentiation and insulin sensitivity.

In vitro: GQ-16 was an effective inhibitor of Cdk5-mediated phosphorylation of PPARγ, exhibiting a Ki value of 160 nM. GQ-16 was specific for PPARγ and possessed no detectable activity when tested for the ability to activate other PPAR subtypes (PPARα or PPARβ/δ) or RXRα. In both NIH-3T3 and C3H10T1/2 cell models with established PPARγ-dependent adipogenesis, GQ-16 displayed reduced the potential of adipogenic [1].

In vivo: In the mouse model of diet-induced obesity and insulin resistance, administration of GQ-16 (20 mg/kg/day) by oral gavage daily blocked HFD-dependent effects on intracellular inflammatory pathways and improved insulin sensitivity. GQ-16 did not elicit increased weight gain [1].

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