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.^1,2,3 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 (Item No. 71740) and 15-deoxy-Δ^12,14-prostaglandin J₂ (Item No. 18570).⁴ Through this action, LG 100754 decreases glucose levels and relieves insulin resistance in mice.^5,4

≥98%

Store at -20℃

CD3159;LGD 100754;UVI2112;

1.Hida, T.,Tai, K.,Tokuhara, N., et al. Existence of retinoic acid-receptor-independent retinoid X-receptor-dependent pathway in myeloid cell function. Jpn. J. Pharmacol. 85(1), 60-69 (2001).

2.Lala, D.S.,Mukherjee, R.,Schulman, I.G., et al. Activation of specific RXR heterodimers by an antagonist of RXR homodimers. Nature 383(6599), 450-453 (1996).

3.Schulman, I.G.,Li, C.,Schwabe, J.W.R., et al. The phantom ligand effect: Allosteric control of transcription by the retinoid X receptor. Genes Dev. 11(3), 299-308 (1997).

4.Forman, B.M. The antidiabetic agent LG100754 sensitizes cells to low concentrations of peroxisome proliferator-activated receptor gamma ligands. J. Biol. Chem. 277(15), 12503-12506 (2002).

5.Cesario, R.M.,Klausing, K.,Razzaghi, H., et al. The rexinoid LG100754 is a novel RXR:PPARγ agonist and decreases glucose levels in vivo. Mol. Endocrinol. 15(8), 1360-1369 (2001).