LXRs (Liver X Receptor α and β) are nuclear receptors that act as ligand-activated transcription factors. LXR activation causes upregulation of genes involved in reverse cholesterol transport (RCT), including ABCA1 and ABCG1 transporters, in macrophage and intestine.LXRα/β are ligand-activated transcription factors of the nuclear hormone receptor superfamily that stimulate transcription of several genes, including ABCA1 and apoE. LXRα and LXRβ respond to the same oxysterol ligands and activate transcription as obligate heterodimeric complexes with retinoid X receptors.Synthetic LXR agonists activate both LXRα and LXRβ, cross the blood-brain barrier, and efficiently induce expression of LXR target genes including ABCA1 and apoE.
||SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
||GW3965 hydrochloride is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.
||LXR-623 is a highly brain-penetrant LXRα-partial/LXRβ-full agonist, with IC50 of 179 and 24 nM for LXR-β and the LXR-α subtype, respectively.
||A potent, highly selective partial LXR agonist with Ki of 14 nM for LXRβ, shows moderate selectivity (5-fold) over LXRα (Ki=68 nM).
||A potent, selective, orally active LXR agonist that recruits the steroid receptor coactivator 1 to human LXRα in a cell-free ligand-sensing assay with an EC50 of 125 nM.
||A novel potent, partial LXRβ-selective agonist (EC50=9 nM) with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays.