1221277-90-2
1221277-90-2 結(jié)構(gòu)式
基本信息
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]-
物理化學性質(zhì)
DMSO:17.46(Max Conc. mg/mL);29.51(Max Conc. mM)
常見問題列表
pIC50: 7 (LXRα), 7.4 (LXRβ)
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 .
One month treatment of GSK2033 does not have significant effects on hepatic triglyceride levels. Plasma triglyceride levels are also unaffected by treatment with GSK2033.