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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-PPAR-GQ-16
GQ-16

Chemical Structure : GQ-16

CAS No.: 870554-67-9

GQ-16 (PPARγ agonist GQ16)

货号: PC-49036Not For Human Use, Lab Use Only.

GQ-16 is a peroxisome proliferator-activated receptor γ (PPARγ) ligand and partial agonist with Ki value of 160 nM, specific for PPARγ with no detectable activity to activate other PPAR subtypes (PPARα or PPARβ/δ) or RXRα.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GQ-16 is a peroxisome proliferator-activated receptor γ (PPARγ) ligand and partial agonist with Ki value of 160 nM, specific for PPARγ with no detectable activity to activate other PPAR subtypes (PPARα or PPARβ/δ) or RXRα.
GQ-16 elicited only approximately one-third of the maximal activation stimulated by rosiglitazone at high concentrations.
GQ-16 is significantly less effective in promoting the interaction between PPARγ and SRC-1 than the TZD troglitazone in in vitro binding studies.
GQ-16 displayed reduced adipogenic potential in both NIH-3T3 and C3H10T1/2 cells, established models of PPARγ-dependent adipogenesis.
GQ-16 improves insulin-signaling components in liver, muscle, and adipose tissue of obese Swiss mice.
GQ-16 improves insulin sensitivity without evoking weight gain and inhibits Cdk5 phosphorylation of PPARγ in vitro.

物理化学性质&存储条件

分子量 418.305
分子式 C19H16BrNO3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(5-bromo-2-methoxy-benzylidene)-3-(4-methyl-benzyl)-thiazolidine-2,4-dione

参考文献

1. Amato AA, et al. J Biol Chem. 2012 Aug 10;287(33):28169-79.

2. Coelho MS, et al. PLoS One. 2016 May 3;11(5):e0154310.

3. da Costa Leite L. F.,et al. Eur. J. Med. Chem. 42, 1263–1271

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