Oliva, Paola; Scortichini, Mirko; Dobelmann, Clemens; Jain, Shanu; Gopinatth, Varun; Toti, Kiran S.; Phung, Ngan B.; Junker, Anna; Jacobson, Kenneth A. published an article in 2021. The article was titled 《Structure-activity relationships of pyrimidine nucleotides containing a 5′-α,β-methylene diphosphonate at the P2Y6 receptor》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Related Products of 1129-28-8 The information in the text is summarized as follows:
The Gq-coupled P2Y6 receptor (P2Y6R) is a component of the purinergic signaling system and functions in inflammatory, cardiovascular and metabolic processes. UDP, the native P2Y6R agonist and P2Y14R partial agonist, is subject to hydrolysis by ectonucleotidases. Therefore, we have synthesized UDP/CDP analogs, e.g. I, containing a stabilizing α,β-methylene bridge as P2Y6R agonists and identified compatible affinity-enhancing pyrimidine modifications. A distal binding region on the receptor was explored with 4-benzyloxyimino CDP analogs and their potency determined in a calcium mobilization assay. A 4-trifluoromethyl-benzyloxyimino substituent provided the highest human P2Y6R potency (MRS4554, 0.57μM), and a 5-fluoro substitution of the cytosine ring similarly enhanced potency, with >175- and 39-fold selectivity over human P2Y14R, resp. However, 3-alkyl, β-D-arabinofuranose, and 6-aza substitution prevented P2Y6R activation. Thus, we have identified new α,β-methylene bridged N4-extended CDP analogs as P2Y6R agonists that are highly selective over the P2Y14R. In the experiment, the researchers used Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Related Products of 1129-28-8)
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. Some of these compounds are identical to man-made organobromine compounds, such as methyl bromide, bromoform, and bromophenols, but many others are entirely new moleclar entities, often possessing extraordinary and important biological properties. Related Products of 1129-28-8
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary