中文名 | GSK 2033 |
英文名 | 2,4,6-Trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]benzenesulfonamide |
英文别名 | GSK 2033 LXR antagonist 2033 2,4,6-Trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]benzenesulfonamide Benzenesulfonamide, 2,4,6-trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]- |
CAS | 1221277-90-2 |
化学式 | C29H28F3NO5S2 |
分子量 | 591.66 |
溶解度 | 溶于DMSO,不溶于水 |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | GSK2033 is a LXR antagonist with pIC 50 s of 7 and 7.4 for LXRα or LXRβ, respectively. GSK2033 dose-dependently suppresses basal transcription in full-length LXRα or full-length LXRβ cotransfection assays with IC 50 s of 17 nM and 9 nM, respectively. GSK2033 also effectively suppresses the transcription of an ABCA1 driven luciferase reporter dose-dependently displaying IC 50 s of 52 nM for LXRα and 10 nM for LXRβ. GSK2033 also suppresses the expression of both of fatty acid synthase ( FASN ) and SREBP1 . |
体内研究 | One month treatment of GSK2033 does not have significant effects on hepatic triglyceride levels. Plasma triglyceride levels are also unaffected by treatment with GSK2033. |
参考资料 展开查看 | 1: Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM. Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J Med Chem. 2010 Apr 22;53(8):3412-6. doi: 10.1021/jm901797p. PubMed PMID: 20345102. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.69 ml | 8.451 ml | 16.902 ml |
5 mM | 0.338 ml | 1.69 ml | 3.38 ml |
10 mM | 0.169 ml | 0.845 ml | 1.69 ml |
5 mM | 0.034 ml | 0.169 ml | 0.338 ml |
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