| Identification | Back Directory | [Name]
GSK3987 | [CAS]
264206-85-1 | [Synonyms]
GSK3987
GSK3987 1-benzyl-3-((4-methoxyphenyl)amino)-4-phenyl-1H-pyrrole-2,5-dione | [Molecular Formula]
C24H20N2O3 | [MOL File]
264206-85-1.mol | [Molecular Weight]
384.43 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [storage]
-20°C | [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)
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| Company Name: |
cjbscvictory
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| Telephone: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
| Company Name: |
Bide Pharmatech Ltd.
|
| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
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