一般描述
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.
生化/生理作用
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
制备说明
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 year at -20°C.
储存分类代码
10-13 - German Storage Class 10 to 13
法规信息
新产品
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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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