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GQ-16

 
Catalog No.
C3407
PPARγ的部分激动剂
组合的产品项目
规格价格库存 数量
10mg
¥ 1,191.00
Ship with 10-15 days
50mg
¥ 4,170.00
Ship with 10-15 days
100mg
¥ 6,337.00
Ship with 10-15 days

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A

背景

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.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt418.3
Cas No.870554-67-9
FormulaC19H16BrNO3S
Solubility≤0.33mg/ml in DMSO;5mg/ml in dimethyl formamide
Chemical Name5Z-[(5-bromo-2-methoxyphenyl)methylene]-3-[(4-methylphenyl)methyl]-2,4-thiazolidinedione
SDFDownload SDF
Canonical SMILESBrC1=CC(/C=C2C(N(CC3=CC=C(C)C=C3)C(S/2)=O)=O)=C(OC)C=C1
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批次:

化学结构

GQ-16