GQ-16

A PPARγ partial agonist

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库存: 现货

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5mg

￥412.00

330.00

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10mg

￥775.00

620.00

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50mg

￥2800.00

2240.00

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100mg

￥4437.00

3550.00

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货号: ajci8074
CAS: 870554-67-9
别名:
分子式: C19H16BrNO3S
分子量: 418.3
纯度: >98%
溶解度: ≤0.33mg/ml in DMSO;5mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

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.