Nomura, Sayaka; Endo-Umeda, Kaori; Makishima, Makoto; Hashimoto, Yuichi; Ishikawa, Minoru published an article in 2016, the title of the article was Development of Tetrachlorophthalimides as Liver X Receptor β (LXRβ)-Selective Agonists.SDS of cas: 157869-15-3 And the article contains the following content:
Liver X receptor (LXR) agonists are candidates for the treatment of atherosclerosis via induction of ABCA1 (ATP-binding cassette A1) gene expression, which contributes to reverse cholesterol transport (RCT) and to cholesterol efflux from the liver and intestine. However, LXR agonists also induce genes involved in lipogenesis, such as SREBP-1c (sterol regulatory binding element protein 1c) and FAS (fatty acid synthase), thereby causing an undesirable increase in plasma and hepatic triglyceride (TG) levels. Recent studies indicate that LXRα contributes to lipogenesis in liver, and selective LXRβ activation improves RCT in mice. Therefore, LXRβ-selective agonists are promising candidates to improve atherosclerosis without increasing plasma or hepatic TG levels. However, the ligand-binding domains in the two LXR isoforms α/β share high sequence identity, and few LXR ligands show subtype selectivity. In this study the authors identified a tetrachlorophthalimide analog as an LXRβ-selective agonist. Structural development led to (E)-4,5,6,7-tetrachloro-2-(2-styrylphenyl)isoindoline-1,3-dione (I), which shows potent and selective LXRβ agonistic activity in reporter gene assays. In binding assays, compound I bound to LXRβ preferentially over LXRα. It also induced the expression of ABCA1 mRNA but not SREBP-1c mRNA in cells. Compound I appears to be a promising lead compound for therapeutic agents to treat atherosclerosis without the side effects induced by LXRα/β dual agonists. The experimental process involved the reaction of 2-((4-Methoxyphenyl)ethynyl)aniline(cas: 157869-15-3).SDS of cas: 157869-15-3
The Article related to tetrachlorophthalimide liver x receptor beta agonist, abca1, srebp-1c, agonists, atherosclerosis, liver x receptor (lxr), Pharmacology: Structure-Activity and other aspects.SDS of cas: 157869-15-3
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