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1221277-90-2

中文名稱 1221277-90-2
英文名稱 GSK 2033
CAS 1221277-90-2
分子式 C29H28F3NO5S2
分子量 591.66
MOL 文件 1221277-90-2.mol
更新日期 2024/12/22 16:36:06
1221277-90-2 結(jié)構(gòu)式 1221277-90-2 結(jié)構(gòu)式

基本信息

中文別名
化合物GSK2033
英文別名
GSK 2033
LXR antagonist 2033
GSK2033 >=98% (HPLC)
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]-

物理化學(xué)性質(zhì)

儲(chǔ)存條件2-8°C
溶解度DMF:5.0(Max Conc. mg/mL);8.45(Max Conc. mM)
DMSO:17.46(Max Conc. mg/mL);29.51(Max Conc. mM)
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335

常見問題列表

生物活性
GSK2033 是一種 LXR 拮抗劑,對(duì)于 LXRα 和 LXRβ 的 pIC50 值分別為 7 和 7.4。
靶點(diǎn)

pIC50: 7 (LXRα), 7.4 (LXRβ)

體外研究

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 .

體內(nèi)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.

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