440165
LXRα/β Agonist - CAS 264206-85-1 - Calbiochem
Synonym(s):
3-((4-Methoxyphenyl)amino)-4-phenyl-1-(phenylmethyl)-1H-pyrrole-2,5-dione
General description
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 LXRα and LXRβ, respectively). Displays >50-fold selectivity for LXR over a panel of nuclear receptors, including FXR, PPARα/γ/δ, PXR, AR, ERα/β, 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.
Biochem/physiol Actions
A potent and specific liver X receptor (LXR) dual agonist
EC50 = 50 nM and 40 nM for the recruitment of SRC1 to LXRα and LXRβ, respectively
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 year at -20°C.
Storage Class Code
10-13 - German Storage Class 10 to 13
Regulatory Information
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Michael C Jaye et al.
Journal of medicinal chemistry, 48(17), 5419-5422 (2005-08-19)
Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a high throughput screen as inducers of human ATP binding cassette transporter A1 expression. Mechanism of action studies led to the identification of GSK3987 as an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to
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