WO95E | PPARγ agonist | Probechem Biochemicals

Chemical Structure : WO95E

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WO95E (PPARγ agonist WO95E)

货号: PC-38250Not For Human Use, Lab Use Only.

WO95E is a novel potent, synthetic ligand (partial agonist) of PPARγ, directly binds to PPARγ with IC50 of 11 nM.

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生物&药学活性

WO95E is a novel potent, synthetic ligand (partial agonist) of PPARγ, directly binds to PPARγ with IC50 of 11 nM.
WO95E's binding affinity is approximately 70-fold lower than that of UHC1 (Journal of Biological Chemistry. 2014;289(38):26618–26629.).
WO95E significantly inhibited the S273 phosphorylation of PPARγ in 3T3-L1 differentiated adipocytes, led to the upregulation of the mRNA levels of a number of the PPARγ phosphorylation-dependent genes, including adiponectin, cycp2f2, Ddx-17, Rarres2, and Selenbp1.
Unlike SR1664 and UHC1, WO95E does not bind to the canonical PPARγ ligand-binding pocket (LBP) containing H3, H3-4 loop, H11 and H12, which full agonist Rosi binds, instead, WO95E binds to the ABP comprising H2′-H3, β-sheet, and the Ω loop.
WO95E improved glucose tolerance and insulin sensitivity in DIO mice.

物理化学性质&存储条件

分子量	504.586
分子式	C32H28N2O4
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	4'-((5-((3-hydroxybenzyl)carbamoyl)-2,3-dimethyl-1H-indol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid

参考文献

1. Wu D, et al. Mol Metab. 2021 Dec;54:101363.

WO95E (PPARγ agonist WO95E)

生物&药学活性

物理化学性质&存储条件

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WO95E (PPARγ agonist WO95E)

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物理化学性质&存储条件

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