您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > GSK3987
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
GSK3987
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK3987图片
CAS NO:264206-85-1
包装:5mg
市场价:6275元

产品介绍
GSK3987 是一种泛 LXRα/β 激动剂,对 LXRα-SRC1 和 LXRβ-SRC1 的 EC50 分别为 50 nM 和 40 nM。
Cas No.264206-85-1
Canonical SMILESO=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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)