LG 100754 is a ligand of retinoid X receptor (RXR) that modulates the activity of RXR dimers. It acts as an antagonist towards RXR homodimers but as an agonist of heterodimers consisting of RXR and retinoic acid receptor (RAR) or PPARs. LG 100754, at 1 μM, is a weak agonist of RXR-PPARγ but strongly enhances signaling through the heterodimer in response to PPARγ ligands, including rosiglitazone and 15-deoxy-Δ12,14-prostaglandin J2 . Through this action, LG 100754 decreases glucose levels and relieves insulin resistance in mice.
