GSK2033

GSK2033 is an antagonist of liver X receptor alpha (LXRalpha) and LXRbeta (IC50s = 0.1 and 0.398 µM, respectively) that has no agonist activity in an LXR transactivation assay. It inhibits LXR agonist-induced and basal expression of the LXR target genes ATP-binding cassette transporter 1 (ABCA1) and sterol regulatory element binding protein 1c (SREBP-1c) in THP-1 and HepG2 cells, respectively. However, GSK2033 binds promiscuously to a variety of nuclear receptors including RORgamma, RXRalpha, ERalpha, and ERbeta in a nuclear receptor specificity assay in HEK293 cells and, in a mouse model of non-alcoholic fatty liver disease (NAFLD), it induces the expression of fatty acid synthase and SREBP-1.Formal Name: 2,4,6-trimethyl-N-[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[[5-(trifluoromethyl)-2-furanyl]methyl]-benzenesulfonamide. CAS Number: 1221277-90-2. Molecular Formula: C29H28F3NO5S2. Formula Weight: 591.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5 mg/ml, DMSO: 3 mg/ml, Ethanol: partially soluble. lambdamax: 255 nm. SMILES: CC1=CC(C)=C(S(N(CC2=CC=C(C3=CC=CC(S(C)(=O)=O)=C3)C=C2)CC4=CC=C(C(F)(F)F)O4)(=O)=O)C(C)=C1. InChi Code: 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. InChi Key: PSOXOVKYGWBTPB-UHFFFAOYSA-N.