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1416153-62-2

中文名稱 1416153-62-2
英文名稱 SR9238
CAS 1416153-62-2
分子式 C31H33NO7S2
分子量 595.73
MOL 文件 1416153-62-2.mol
1416153-62-2 結(jié)構(gòu)式 1416153-62-2 結(jié)構(gòu)式

基本信息

中文別名
化合物SR9238
5-((2,4,6-三甲基-N-((3'-(甲基磺?;?-[1,1'-聯(lián)苯]-4-基)甲基)苯磺酰胺基)甲基)呋喃-2-羧酸乙酯
英文別名
SR9238
SR9238 >=98% (HPLC)
SR9238
SR-9238
SR 9238
Ethyl 5-[[[[3'-(Methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl][(2,4,6-trimethylphenyl)sulfonyl]amino]methyl]-2-furancarboxylate
2-Furancarboxylic acid, 5-[[[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl][(2,4,6-trimethylphenyl)sulfonyl]amino]methyl]-, ethyl ester

物理化學(xué)性質(zhì)

沸點(diǎn)787.7±70.0 °C(Predicted)
密度1.268±0.06 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度DMF: 5 mg/ml; DMF:PBS(pH7.2) (1:2): 0.3 mg/ml; DMSO: 5 mg/ml
酸度系數(shù)(pKa)-10.53±0.70(Predicted)
形態(tài)粉末
顏色白色至米色
1416153-62-2價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-1014421416153-62-2
SR9238
1416153-62-25mg770元
2024/11/08HY-1014421416153-62-2
SR9238
1416153-62-210mM * 1mLin DMSO1009元
2024/11/08HY-1014421416153-62-2
SR9238
1416153-62-210mg1350元

常見問題列表

生物活性
SR9238 是一種合成的肝 X 受體 (LXR) 反向激動(dòng)劑,對(duì)于 LXRα 和 LXRβ 的 IC50 值分別為 214 nM 和 43 nM。
靶點(diǎn)

IC50: 43 nM (LXRβ), 214 nM (LXRα)

體外研究

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.

體內(nèi)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.

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