GSK3987 is a pan LXRα/β agonist with EC 50 s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation.
性状
Solid
IC50 & Target[1][2]
EC50: 50 nM (LXRα); 40 nM (LXRβ)
体外研究(In Vitro)
GSK3987 (compound 4) shows activity with EC50s of 0.08 μM, 50 nM, 40 nM for ABCA1, LXRα-SRC1, LXRβ-SRC1, respectively.GSK3987 (30, 100, 300, 1000 nM) increases the expression of ABCA1 and induces cellular cholesterol efflux to apoA1 particles in a dose-dependent manner in primary human macrophages.GSK3987 (6-1500 nM) increases the expression of SREBP-1c and induces triglyceride accumulation in human hepatoma (HepG2) cells in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.