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
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)
GSK3987 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK3987 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Nanjing Doge Biomedical Technology Co., Ltd | +86-25-58227606 +86-15305155328 | sales@dogechemical.com | China | 4128 | 58 |
Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 5225 | 58 |
Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9806 | 58 |
Shanghai Han-Xiang Chemical Co., Ltd. | 15971444841 | amber@biochempartner.com | China | 3063 | 58 |
DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9412 | 58 |
ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |