Patch, Raymond J. published the artcileIdentification of Diaryl Ether-Based Ligands for Estrogen-Related Receptor α as Potential Antidiabetic Agents, HPLC of Formula: 220141-23-1, the publication is Journal of Medicinal Chemistry (2011), 54(3), 788-808, database is CAplus and MEDLINE.
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.
Journal of Medicinal Chemistry published new progress about 220141-23-1. 220141-23-1 belongs to esters-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Benzene,Ester, name is Methyl 4-fluoro-2-(trifluoromethyl)benzoate, and the molecular formula is C9H6F4O2, HPLC of Formula: 220141-23-1.
Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics