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GQ-16
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GQ-16图片
CAS NO:870554-67-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
GQ-16 是 PPARγ 的配体结合域 (LBD) 的中等亲和力配体,其 Ki 值为 160 nM。
Cas No.870554-67-9
化学名5Z-[(5-bromo-2-methoxyphenyl)methylene]-3-[(4-methylphenyl)methyl]-2,4-thiazolidinedione
Canonical SMILESBrC1=CC(/C=C2C(N(CC3=CC=C(C)C=C3)C(S/2)=O)=O)=C(OC)C=C1
分子式C19H16BrNO3S
分子量418.3
溶解度≤0.33mg/ml in DMSO;5mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.