GSK3987

Names

[ Name ]:
GSK3987

[Synonym ]:
1-Benzyl-3-[(4-methoxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
1-BENZYL-3-(4-METHOXYPHENYLAMINO)-4-PHENYLPYRROLE-2,5-DIONE
1H-Pyrrole-2,5-dione, 3-[(4-methoxyphenyl)amino]-4-phenyl-1-(phenylmethyl)-

Biological Activity

[Description]:

GSK3987 is a pan LXRα/β agonist with EC50s 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[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> LXR

Research Areas >> Metabolic Disease

[Target]

EC50: 50 nM (LXRα); 40 nM (LXRβ)[1]

[In Vitro]

GSK3987 (compound 4) shows activity with EC50s of 0.08 µM, 50 nM, 40 nM for ABCA1, LXRα-SRC1, LXRβ-SRC1, respectively[1]. 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[1]. GSK3987 (6-1500 nM) increases the expression of SREBP-1c and induces triglyceride accumulation in human hepatoma (HepG2) cells in a dose-dependent manner[1]. RT-PCR[1] Cell Line: HepG2 cells Concentration: 6-1500 nM Incubation Time: Result: Increased the expression of SREBP-1c and induced triglyceride accumulation in human hepatoma (HepG2) cells in a dose-dependent manner.

[References]

[1]. HepG2 cells, ABCA1, SREBP-1c, cellular cholesterol, macrophages, triglyceride accumulation

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
572.4±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₀N₂O₃

[ Molecular Weight ]:
384.427

[ Flash Point ]:
299.9±30.1 °C

[ Exact Mass ]:
384.147400

[ LogP ]:
4.35

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.684

[ Storage condition ]:
2-8°C