GSK3987
- CAS No.
- 264206-85-1
- Chemical Name:
- GSK3987
- Synonyms
- GSK3987;LXRα/β Agonist;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
- Molecular Weight:
- 384.43
- MDL Number:
- MOL File:
- 264206-85-1.mol
GSK3987 Chemical Properties,Uses,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
GSK3987 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 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 | 8467 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 5221 | 58 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |
| Shanghai Han-Xiang Chemical Co., Ltd. | 15971444841 | amber@biochempartner.com | China | 3061 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9409 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11218 | 58 |
