LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR^[1]. In Vitro: LG100754 is a selective activator of endogenous RXR heterodimers^[1].
LG100754 can also improve TNFα-mediated insulin resistance in mature adipocytes^[1].
LG100754 acts as a bona fide activator of endogenous RXR:PPARγ heterodimers and regulator of insulin-dependent signaling pathways^[1].
In Vivo: LG100754 (100 mg/kg) completely blocks the increase in glucose levels, suggesting that LG100754 can improve insulin resistance in vivo^[1].