| CAS NO: | 264206-85-1 |
| 包装: | 5mg |
| 市场价: | 6275元 |
| Cas No. | 264206-85-1 |
| Canonical SMILES | O=C(N1CC2=CC=CC=C2)C(C3=CC=CC=C3)=C(NC4=CC=C(OC)C=C4)C1=O |
| 分子式 | C24H20N2O3 |
| 分子量 | 384.4 |
| 溶解度 | DMSO: 200 mg/ml,Methanol: 100 mg/ml |
| 储存条件 | -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | GSK3987 is a dual agonist of liver X receptor α (LXRα) and LXRβ.1It 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 induceABCA1expression 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. 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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