Formulation: A solid
Formal Name: 3-[(4-methoxyphenyl)amino]-4-phenyl-1-(phenylmethyl)-1H-pyrrole-2,5-dione
Purity: ≥98%
Formula Markup: C24H20N2O3
Formula Weight: 384,4
Shelf life (days): 1460
CAS Number: 264206-85-1
Notes: GSK3987 is a dual agonist of liver X receptor α (LXRα) and LXRβ.{57442} It recruits steroid receptor coactivator 1 (SRC-1) to LXRα and LXRβ in a ligand-sensing assay (LiSA; EC50s = 50 and 40 nM, respectively). GSK3987 is 50-fold selective for LXRα and LXRβ over a panel of nuclear receptors and GSK3β (IC50 = >5,000 nM) but does induce ABCA1 expression in a reporter assay using THP-1 cells (EC50 = 80 nM). It inhibits LPS-induced IL-6 secretion in THP-1 macrophages. GSK3987 increases the expression of the sterol regulatory element binding protein 1c (SREBP-1c) and induces triglyceride accumulation in HepG2 cells in a concentration-dependent manner.
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