Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines

…, KD Plunket, DG Morgan, EJ Beaudet…

文献索引：Collins, Jon L.; Binz, Jane G.; Plunket, Kelli D.; Morgan, Daniel G.; Beaudet, Elizabeth J.; Whitney, Karl D.; Kliewer, Steven A.; Willson, Timothy M.; Fivush, Adam M.; Watson, Michael A.; Galardi, Cristin M.; Lewis, Michael C.; Moore, Linda B.; Parks, Derek J.; Wilson, Joan G.; Tippin, Tim K. Journal of Medicinal Chemistry, 2002 , vol. 45, # 10 p. 1963 - 1966

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被引用次数: 361

摘要

A potent, selective, orally active LXR agonist was identified from focused libraries of tertiary amines. GW3965 (12) recruits the steroid receptor coactivator 1 to human LXRα in a cell-free ligand-sensing assay with an EC50 of 125 nM and profiles as a full agonist on hLXRα and hLXRβ in cell-based reporter gene assays with EC50's of 190 and 30 nM, respectively. After oral dosing at 10 mg/kg to C57BL/6 mice, 12 increased expression of the reverse ...