LG100754

LG100754 is a **synthetic rexinoid ligand** with selective modulatory activity at retinoid X receptor (RXR) dimers. LG100754 acts as a **full antagonist of RXR homodimers** and as a **selective agonist for RXR:PPARγ and RXR:PPARα heterodimers**, thereby modulating nuclear receptor signaling related to metabolism and gene transcription[1][2][3][4][5][7][8]. It does not activate other RXR heterodimers such as RXR:liver X receptor or RXR:farnesoid X receptor, making it distinct from other RXR ligands[3]. LG100754 also demonstrates a unique effect termed the “phantom effect,” where it binds RXR within RAR/RXR heterodimers and activates RAR-mediated transcription via SRC-1 coactivator recruitment, affecting metabolic and cancer-related pathways[1][2][4]. Preclinical studies show LG100754 ameliorates insulin resistance and promotes adipocyte differentiation, indicating potential as a novel insulin sensitizer[3][8]. It is used primarily in research and is not an approved medication.

Other names

(2E,4E,6Z)-3-Methyl-7-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-propoxy-2-naphthalenyl)-2,4,6-Octatrienoic acid