GSK3987 是一种泛 LXRα/β 激动剂，对 LXRα-SRC1 和 LXRβ-SRC1 的 EC50 分别为 50 nM 和 40 nM。
货号:ajcx24350
CAS:264206-85-1
分子式:C24H20N2O3
分子量：384.4
溶解度:DMSO: 200 mg/ml,Methanol: 100 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GSK3987 is a dual agonist of liver X receptor α (LXRα) and LXRβ.¹It 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 induceABCA1expression 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.

1.Jaye, M.C., Krawiec, J.A., Campobasso, N., et al.Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structureJ. Med. Chem.48(17)5419-5422(2005)