3-((4-Methoxyphenyl)amino)-4-phenyl-1-(phenylmethyl)-1H-pyrrole-2,5-dione Orange solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable maleimide analog that acts as a potent and specific liver X receptor (LXR) dual agonist (EC50 = 50 nM and 40 nM for the recruitment of SRC1 to LXRa and LXRb, respectively). Displays >50-fold selectivity for LXR over a panel of nuclear receptors, including FXR, PPARa/g/d, PXR, AR, ERa/b, GR, and PR. Upregulates ABCA1-dependent transcriptional activity (EC50 = 80 nM) and inhibits LPS-stimulated secretion of the proinflammatory cytokine, IL-6, in THP-1 cells. Purity: ≥98% by HPLC. Ref.: Jaye, M.C., et al. 2005. J. Med. Chem. 48, 5419. |
