SR 1078

SR-1078 is a selective agonist of RORα and RORγ that stimulates ROR transcriptional activity in HEK293 cell reporter assays at concentrations as low as 2 μM without effect at the related liver X receptors and farnesoid X receptors. SR1078 modulates the conformation of RORγ in a biochemical assay and activates RORα and RORγ driven transcription. SR1078 stimulates expression of endogenous ROR target genes in HepG2 cells that express both RORα and RORγ. SR1078 can be utilized as a chemical tool to probe the function of these receptors both in vitro and in vivo.