GSK-2945 is a potent and selective small molecule Rev-Erbα agonist with EC50 of 50 nM, displays >1,000-fold selectivity over LXRα; inhibits LPS induction of IL-6 production and to upregulate expression of ABCA1 in human THP-1 cells; demonstrates in vivo bioavailability and orally active.

SR12418 is a REV-ERB-specific synthetic ligand with IC50s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research.