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GSK3987

CAS No.
264206-85-1
Chemical Name:
GSK3987
Synonyms
GSK3987;LXRα/β Agonist;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
Molecular Weight:
384.43
MDL Number:
MOL File:
264206-85-1.mol
Last updated:2024-07-02 08:54:57

GSK3987 Properties

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

GSK3987 Chemical Properties,Uses,Production

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)

264206-68-0
100-51-6
264206-85-1
Synthesis of GSK3987 from 1H-Pyrrole-2,5-dione, 3-[(4-methoxyphenyl)amino]-4-phenyl- and Benzyl alcohol

GSK3987 Preparation Products And Raw materials

Raw materials

Preparation Products

GSK3987 Suppliers

Global( 25)Suppliers
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TargetMol Chemicals Inc.
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Nanjing Doge Biomedical Technology Co., Ltd
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Wuhan Topule Biopharmaceutical Co., Ltd
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Aladdin Scientific
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Wuhan Jingkang en Biomedical Technology Co., Ltd
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Shanghai EFE Biological Technology Co., Ltd. 021-65675885 18964387627 info@efebio.com China 9806 58
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DC Chemicals 021-58447131 13564518121 sales@dcchemicals.com China 9412 58
ChemeGen(Shanghai) Biotechnology Co.,Ltd. 18818260767 sales@chemegen.com China 11289 58
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 264206-85-1