GSK3987

Product Name: GSK3987
CAS No.: 264206-85-1
Chemical Name: GSK3987
Synonyms: GSK3987;LXRα/β Agonist;GSK3987 ，E0099;GSK3987, 10 mM in DMSO;1-Benzyl-3-((4-methoxyphenyl)amino)-4-phenyl-1H-pyrrole-2,5-dione;GSK3987 1-benzyl-3-((4-methoxyphenyl)amino)-4-phenyl-1H-pyrrole-2,5-dione;1H-Pyrrole-2,5-dione, 3-[(4-methoxyphenyl)amino]-4-phenyl-1-(phenylmethyl)-;macrophages,GSK 3987,cellular cholesterol,inhibit,ABCA1,HepG2 cells,Inhibitor,SREBP-1c,LXR,Liver X receptor,triglyceride accumulation,GSK3987,GSK-3987
CBNumber: CB02669287
Molecular Formula: C24H20N2O3
Formula Weight: 384.43
MOL File: 264206-85-1.mol

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GSK3987 Property

Boiling point:: 572.4±50.0 °C(Predicted)
Density: 1.309±0.06 g/cm3(Predicted)
storage temp.: -20°C
solubility: DMSO: 200 mg/ml,Methanol: 100 mg/ml
form: A solid
pka: -1.27±0.20(Predicted)
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

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GSK3987 Chemical Properties,Usage,Production

Uses

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].

Biological Activity

GSK3987 is a dual agonist of liver X receptor α (LXRα) and LXRβ.1 It 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 induce ABCA1 expression 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.

References

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)

GSK3987 Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK3987 Suppliers

China 34 United States 3 Global 37

Shanghai EFE Biological Technology Co., Ltd.

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264206-85-1, GSK3987Related Search:

GSK3987

GSK3987 1-benzyl-3-((4-methoxyphenyl)amino)-4-phenyl-1H-pyrrole-2,5-dione

macrophages,GSK 3987,cellular cholesterol,inhibit,ABCA1,HepG2 cells,Inhibitor,SREBP-1c,LXR,Liver X receptor,triglyceride accumulation,GSK3987,GSK-3987

1H-Pyrrole-2,5-dione, 3-[(4-methoxyphenyl)amino]-4-phenyl-1-(phenylmethyl)-

LXRα/β Agonist

1-Benzyl-3-((4-methoxyphenyl)amino)-4-phenyl-1H-pyrrole-2,5-dione

GSK3987, 10 mM in DMSO

GSK3987 ，E0099

264206-85-1