产品描述:
GSK2033 is an antagonist of liver X receptor α (LXRα) and LXRβ (IC50s = 0.1 and 0.398 µM, respectively) that has no agonist activity in an LXR transactivation assay.{36795} 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 RORγ, RXRα, ERα, and ERβ 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.{36796}