In 2022,Lagu, Bharat; Wu, Xinyuan; Kulkarni, Santosh; Paul, Rakesh; Becherer, J. David; Olson, Lyndsay; Ravani, Stella; Chatzianastasiou, Athanasia; Papapetropoulos, Andreas; Andrzejewski, Sylvia published an article in Journal of Medicinal Chemistry. The title of the article was 《Orally Bioavailable Enzymatic Inhibitor of CD38, MK-0159, Protects against Ischemia/Reperfusion Injury in the Murine Heart》.Related Products of 27489-62-9 The author mentioned the following in the article:
CD38 is one of the major NAD (NAD+)- and NADP (NADP+)-consuming enzymes in mammals. NAD+, NADP+, and their reduced counterparts are essential coenzymes for numerous enzymic reactions, including the maintenance of cellular and mitochondrial redox balance. CD38 expression is upregulated in age-associated inflammation as well as numerous metabolic diseases, resulting in cellular and mitochondrial dysfunction. Recent literature studies demonstrate that CD38 is activated upon ischemia/reperfusion (I/R), leading to a depletion of NADP+, which results in endothelial damage and myocardial infarction in the heart. Despite increasing evidence of CD38 involvement in various disease states, relatively few CD38 enzymic inhibitors have been reported to date. Herein, we describe a CD38 enzymic inhibitor (MK-0159, IC50 = 3 nM against murine CD38) that inhibits CD38 in in vitro assay. Mice treated with MK-0159 (I) show strong protection from myocardial damage upon cardiac I/R injury compared to those treated with NAD+ precursors (nicotinamide riboside) or the known CD38 inhibitor, 78c. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Related Products of 27489-62-9)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Related Products of 27489-62-9
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