1416153-62-2

中文名称:

1416153-62-2

中文同义词:

英文名称:

SR9238

英文同义词:

SR9238;Ethyl 5-[[[[3-(Methylsulfonyl)[1,1-biphenyl]-4-yl]methyl][(2,4,6-trimethylphenyl)sulfonyl]amino]methyl]-2-furancarboxylate;SR9238;SR-9238;SR 9238;2-Furancarboxylic acid, 5-[[[[3-(methylsulfonyl)[1,1-biphenyl]-4-yl]methyl][(2,4,6-trimethylphenyl)sulfonyl]amino]methyl]-, ethyl ester;SR9238 >=98% (HPLC)

CAS号:

1416153-62-2

分子式:

C31H33NO7S2

分子量:

595.73

EINECS号:

相关类别:

API

Mol文件:

1416153-62-2.mol

沸点 

787.7±70.0 °C(Predicted)

密度 

1.268±0.06 g/cm3(Predicted)

储存条件 

2-8°C

形态

powder

酸度系数(pKa)

-10.53±0.70(Predicted)

颜色

white to beige

生物活性

SR9238 是一种合成的肝 X 受体 (LXR) 反向激动剂，对于 LXRα 和 LXRβ 的 IC50 值分别为 214 nM 和 43 nM。

靶点

IC50: 43 nM (LXRβ), 214 nM (LXRα)

体外研究

Results from the cell-based cotransfection assays demonstrate that SR9238 is a synthetic LXR inverse agonist with IC 50 s of 214 nM and 43 nM for LXRα and LXRβ, respectively. SR9238 also effectively suppresses transcription from a fatty acid synthase ( Fasn ) promoter driven luciferase reporter. It is found that SR9238 induces increased interaction of CoRNR box peptides derived from NCoR (NCoR ID1 and NCoR ID2) with both LXRα and LXRβ, while causing decreased interaction with a coactivator NR box peptide derived from TRAP220. SR9238-induced recruitment of CoRNR box peptides is dose-dependent for both LXRα and LXRβ. HepG2 cells treated with SR9238 result in a significant decrease in Fasn and Srebp1c mRNA expression.

体内研究

Approximately 6 μM SR9238 is detected in the liver 2h after the injection of SR9238, but no compound is detected in the plasma. SR9238 is also detected in the intestine with either ip or oral administration. SR9238-treated mice display greatly reduced lipid content in the liver. Results demonstrate that both Tnfa and Il1b expression are substantially reduced (~80% and >95%, respectively) in the SR9238-treated mice when compare to the vehicle-treated mice. SR9238-treated DIO mice display considerably lower intensity of F4/80 staining versus vehicle-treated DIO mice consistent with a beneficial effect of SR9238 on non-alcoholic steatohepatitis (NASH). SR9238 treatment does not alter body weight or percent body fat composition relative to vehicle treated animals during the experiment. Treatment with SR9238 suppresses diet-induced hepatosteatosis, hepatic inflammation, and hepatocellular injury.