Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 122-07-6, Name is 2,2-Dimethoxy-N-methylethanamine, SMILES is COC(CNC)OC, belongs to amides-buliding-blocks compound. In a document, author is Back, Jan O., introduce the new discover, Name: 2,2-Dimethoxy-N-methylethanamine.
Discovery of tetrahydroquinolines and benzomorpholines as novel potent ROR gamma t agonists
The retinoic acid receptor-related orphan receptor gamma t (ROR gamma t) is an important nuclear receptor that regulates the differentiation of Th17 cells and production of interleukin 17(IL-17). ROR gamma t agonists increase basal activity of ROR gamma t and could provide a potential approach to cancer immunotherapy. Herein, hit compound 1 was identified as a weak ROR gamma t agonist during in-house library screening. Changes in LHS core of 1 led to the identification of tetrahydroquinoline compound 6 as a partial ROR gamma t agonist (max. act. = 39.3%). Detailed structure-activity relationship on substituent of the LHS core, amide linker and RHS arylsulfonyl moiety was explored and a novel series of tetrahydroquinolines and benzomorpholines was discovered as potent ROR gamma t agonists. Tetrahydroquinoline compound 8g (EC50 = 8.9 +/- 0.4 nM, max. act. = 104.5%) and benzomorpholine compound 9g (EC50 = 7.5 +/- 0.6 nM, max. act. = 105.8%) were representative compounds with high ROR gamma t agonistic activity in dual FRET assay, and they showed good activity in cell-based Gal4 reporter gene assay and Th17 cell differentiation assay (104.5% activation at 300 nM of 8g; 59.4% activation at 300 nM of 9g). The binding modes of 8g and 9g as well as the two ROR gamma t inverse agonists accidentally discovered were also discussed. (C) 2020 Elsevier Masson SAS. All rights reserved.
The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 122-07-6 is helpful to your research. Name: 2,2-Dimethoxy-N-methylethanamine.