GSK3987 是广谱LXRα/β激动剂，EC50分别为 50 nM 和 40 nM。GSK3987增加 ABCA1 和 SREBP-1c 蛋白的表达，诱导细胞甘油三酯的积累和胆固醇流出。

GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.

In primary human macrophages, GSK3987 (30, 100, 300, 1000 nM) increased the expression of ABCA1 and induces cellular cholesterol efflux to apoA1 particles in a dose-dependent manner. In human hepatoma (HepG2) cells, GSK3987 (6-1500 nM) increases the expression of SREBP-1c and induces triglyceride accumulation in a dose-dependent manner[1]. GSK3987 showed activity with EC50s of 0.08 μM, 50 nM, 40 nM for ABCA1, LXRα-SRC1, LXRβ-SRC1, respectively[1].

264206-85-1

C24H20N2O3

384.43

DMSO:50 mg/ml (130.06 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years