ChemicalBook > CAS DataBase List > GSK3987
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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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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