Yamada, Shoya;Kawasaki, Mayu;Fujihara, Michiko;Watanabe, Masaki;Takamura, Yuta;Takioku, Maho;Nishioka, Hiromi;Takeuchi, Yasuo;Makishima, Makoto;Motoyama, Tomoharu;Ito, Sohei;Tokiwa, Hiroaki;Nakano, Shogo;Kakuta, Hiroki published 《Competitive Binding Assay with an Umbelliferone-Based Fluorescent Rexinoid for Retinoid X Receptor Ligand Screening》 in 2019. The article was appeared in 《Journal of Medicinal Chemistry》. They have made some progress in their research.Recommanded Product: 2,5-Dimethyl-2,5-hexanediol The article mentions the following:
Ligands for retinoid X receptors (RXRs), “rexinoids”, are attracting interest as candidates for therapy of type 2 diabetes and Alzheimer’s and Parkinson’s diseases. However, current screening methods for rexinoids are slow and require special apparatus or facilities. Here, we created 7-hydroxy-2-oxo-6-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-2H-chromene-3-carboxylic acid (10, CU-6PMN) as a new fluorescent RXR agonist and developed a screening system of rexinoids using 10. Compound 10 was designed based on the fact that umbelliferone emits strong fluorescence in a hydrophilic environment, but the fluorescence intensity decreases in hydrophobic environments such as the interior of proteins. The developed assay using 10 enabled screening of rexinoids to be performed easily within a few hours by monitoring changes of fluorescence intensity with widely available fluorescence microplate readers, without the need for processes such as filtration. The experimental procedure involved many compounds, such as 2,5-Dimethyl-2,5-hexanediol (cas: 110-03-2) .
2,5-Dimethyl-2,5-hexanediol(cas:110-03-2) on heteropoly acid catalyzed dehydration yields cyclic ethers via stereospecific intramolecular SN2 mechanism. It reacts with nitriles in concentrated sulfuric acid to yield Δ1-pyrrolines.Recommanded Product: 2,5-Dimethyl-2,5-hexanediol
Reference:
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