LG101506 (LG1506) is a potent, selective and orally active RXR modulator with Ki of 2.6 nM.
LG101506 binds RXRalpha and activates RXR homo and heterodimers.
LG1506 is a potent insulin sensitizer that also enhances the insulin-sensitizing activities of rosiglitazone.
Administration of LG1506 reduces both body weight gain and food consumption and blocks the TZD-induced weight gain when coadministered with rosiglitazone.
LG1506 does not significantly suppress the thyroid hormone axis in rats, nor does it elevate triglycerides in Sprague Dawley rats.
LG1506 elevates high-density lipoprotein cholesterol in humanized apolipoprotein A-1-transgenic mice.
