GQ-16 |
| Catalog No.GC11916 |
GQ-16 es un ligando de afinidad moderada por el dominio de uniÓn al ligando (LBD) de PPARγ, que exhibe una Ki de 160 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 870554-67-9
Sample solution is provided at 25 µL, 10mM.
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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].
Reference:
[1] Amato A A, Rajagopalan S, Lin J Z, et al. GQ-16, a novel peroxisome proliferator-activated receptor γ (PPARγ) ligand, promotes insulin sensitization without weight gain[J]. Journal of Biological Chemistry, 2012, 287(33): 28169-28179.
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