LXRα/β Agonist is a cell-permeable maleimide analog which acts as a potent and specific LXR (liver X receptor) dual agonist (EC50= 50 nM and 40 nM for the recruitment of SRC1 to LXRα and LXRβ, respectively). It displays >50-fold selectivity for LXR over a panel of nuclear receptors, which include FXR, PPARα/γ/δ, PXR, AR, ERα/β, GR, and PR. This upregulates ABCA1-dependent transcriptional activity (EC50 = 80 nM) as well as inhibits LPS-stimulated secretion of the proinflammatory cytokine, IL-6, in THP-1 cells.
Jaye, M.C., et al. 2005. J. Med. Chem. 48, 5419.
Soluble in DMSO (200 mg/ml), and methanol (100 mg/ml).
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An increase in SREBPAn increase in SREBP-1 protein expression was observed by WB when comparing untreated Hep G2 cells with those that have been treated with LXR / Agonist. -SCBT QC
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