1416153-62-2
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- CAS号:
- 1416153-62-2
- 英文名:
- SR9238
- 英文别名:
- SR9238;SR9238 >=98% (HPLC);SR9238;SR-9238;SR 9238;Liver X receptor,SR-9238,SR 9238,LXR,SR9238,inhibit,Inhibitor;Ethyl 5-(((2,4,6-trimethyl-N-((3'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)phenyl)sulfonamido)methyl)furan-2-carboxylate;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
- 中文名:
- 1416153-62-2
- 中文别名:
- 化合物SR9238;SR 9238,LXR反向激动剂;5-((2,4,6-三甲基-N-((3'-(甲基磺酰基)-[1,1'-联苯]-4-基)甲基)苯磺酰胺基)甲基)呋喃-2-羧酸乙酯
- CBNumber:
- CB43152748
- 分子式:
- C31H33NO7S2
- 分子量:
- 595.73
- MOL File:
- 1416153-62-2.mol
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1416153-62-2化学性质
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沸点:
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787.7±70.0 °C(Predicted)
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密度:
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1.268±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMF: 5 mg/ml; DMF:PBS(pH7.2) (1:2): 0.3 mg/ml; DMSO: 5 mg/ml
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酸度系数(pKa):
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-10.53±0.70(Predicted)
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形态:
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powder
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颜色:
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white to beige
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1416153-62-2性质、用途与生产工艺
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。
IC50: 43 nM (LXRβ), 214 nM (LXRα)
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.
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.
1416153-62-2
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-101442 | 1416153-62-2 SR9238 | 1416153-62-2 | 5mg | 770元 |
2024/04/30 | HY-101442 | 1416153-62-2 SR9238 | 1416153-62-2 | 10mM * 1mLin DMSO | 1009元 |
1416153-62-2, 1416153-62-2 相关搜索:
- API
- 合成有机化合物配体
- C31H33NO7S2
- SR 9238,LXR反向激动剂
- 化合物SR9238
- 5-((2,4,6-三甲基-N-((3'-(甲基磺酰基)-[1,1'-联苯]-4-基)甲基)苯磺酰胺基)甲基)呋喃-2-羧酸乙酯
- 1416153-62-2
- Ethyl 5-(((2,4,6-trimethyl-N-((3'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)phenyl)sulfonamido)methyl)furan-2-carboxylate
- Liver X receptor,SR-9238,SR 9238,LXR,SR9238,inhibit,Inhibitor
- SR9238 >=98% (HPLC)
- 2-Furancarboxylic acid, 5-[[[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl][(2,4,6-trimethylphenyl)sulfonyl]amino]methyl]-, ethyl ester
- SR9238;SR-9238;SR 9238
- Ethyl 5-[[[[3'-(Methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl][(2,4,6-trimethylphenyl)sulfonyl]amino]methyl]-2-furancarboxylate
- SR9238