Identification of Diaryl Ether-Based Ligands for Estrogen-Related Receptor α as Potential Antidiabetic Agents was written by Patch, Raymond J.;Searle, Lily L.;Kim, Alexander J.;De, Debyendu;Zhu, Xizhen;Askari, Hossein B.;O’Neill, John C.;Abad, Marta C.;Rentzeperis, Dionisios;Liu, Jianying;Kemmerer, Michael;Lin, Ling;Kasturi, Jyotsna;Geisler, John G.;Lenhard, James M.;Player, Mark R.;Gaul, Micheal D.. And the article was included in Journal of Medicinal Chemistry in 2011.Recommanded Product: Methyl 3-bromo-4-fluorobenzoate This article mentions the following:
Estrogen-related receptor α (ERRα) is an orphan nuclear receptor that has been functionally implicated in the regulation of energy homeostasis. Herein is described the development of diaryl ether based thiazolidenediones, which function as selective ligands against this receptor. Series optimization provided several potent analogs that inhibit the recruitment of a coactivator peptide fragment in in vitro biochem. assays (IC50 < 150 nM) and cellular two-hybrid reporter assays against the ligand binding domain (IC50 = 1-5 μM). A cocrystal structure of the ligand-binding domain of ERRα with lead compound 29 (I) revealed the presence of a covalent interaction between the protein and ligand, which has been shown to be reversible. In diet-induced murine models of obesity and in an overt diabetic rat model, oral administration of 29 normalized insulin and circulating triglyceride levels, improved insulin sensitivity, and was body weight neutral. This provides the first demonstration of functional activities of an ERRα ligand in metabolic animal models. In the experiment, the researchers used many compounds, for example, Methyl 3-bromo-4-fluorobenzoate (cas: 82702-31-6Recommanded Product: Methyl 3-bromo-4-fluorobenzoate).
Methyl 3-bromo-4-fluorobenzoate (cas: 82702-31-6) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Recommanded Product: Methyl 3-bromo-4-fluorobenzoate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary