GSK3987

LXRα和LXRβ的双重激动剂；在LiSA中募集SRC-1至LXRα和LXRβ（EC50s分别为50和40nM）；对LXRα和LXRβ的选择性是一组核受体和GSK3β的50倍（IC50=>5,000nM），但在使用THP-1细胞的报告检测中诱导ABCA1表达（EC50=80nM）；增加SREBP-1c表达并诱导HepG2细胞中的甘油三酯积累。A dual agonist of LXRα and LXRβ; recruits SRC-1 to LXRα and LXRβ in a LiSA (EC50s = 50 and 40 nM, respectively); 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); increases SREBP-1c expression and induces triglyceride accumulation in HepG2 cells.分子式C24H20N2O3分子量384.4O=C(N1CC2=CC=CC=C2)C(C3=CC=CC=C3)=C(NC4=CC=C(OC)C=C4)C1=O