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GSK 2033
- Soluble in DMSO
- MF: C29H28F3NO5S2
- MW: 591.66
Description
GSK 2033 is a potent, cell-active liver X receptor (LXR) antagonist with an IC50 value of 31.6 nM for LXRβ binding. In LXR agonist-stimulated cells, it reduces expression of ABCA1 in THP-1 cells and SREBP-1c in HepG2 cells.
LXR nuclear receptors regulate cholesterol efflux, lipogenesis and inflammatory metabolic responses. GSK 2033 is a useful chemical probe for studying LXR antagonist pharmacology and LXR-regulated gene expression.
Key Features
- Potent cell-active LXR antagonist
- IC50: 31.6 nM for LXRβ binding
- Reduces ABCA1 expression in THP-1 cells
- Reduces SREBP-1c expression in HepG2 cells
Applications
- LXR nuclear receptor research
- Cholesterol efflux and ABCA1 studies
- Lipid metabolism assays
- Nuclear receptor antagonist profiling
More Information
| Parent CAS No. | 1221277-90-2 |
|---|---|
| Chemical Name | 2,4,6-trimethyl-N-((3'-(methylsulfonyl)biphenyl-4-yl)methyl)-N-((5-(trifluoromethyl)furan-2-yl)methyl)benzenesulfonamide |
| SMILES | C1(S(C)(=O)=O)C=C(C2C=CC(CN(S(C3C(C)=CC(C)=CC=3C)(=O)=O)CC3=CC=C(C(F)(F)F)O3)=CC=2)C=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C29H28F3NO5S2/c1-19-14-20(2)28(21(3)15-19)40(36,37)33(18-25-12-13-27(38-25)29(30,31)32)17-22-8-10-23(11-9-22)24-6-5-7-26(16-24)39(4,34)35/h5-16H,17-18H2,1-4H3 |
| InChiKey | PSOXOVKYGWBTPB-UHFFFAOYSA-N |
| CID | 46203250 |
| Short Description | LXR antagonist |
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