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MGS84 is a novel, cell-impermeable small molecule extracellular nicotinamide phosphoribosyltransferase (eNAMPT) modulator. It is designed to promote and stabilize the dimerization of eNAMPT, thereby increasing its NAD-biosynthetic enzymatic activity and reducing the levels of the pro-inflammatory monomeric form of eNAMPT. In preclinical studies, MGS84 has been shown to reverse the deleterious effects of monomeric eNAMPT, such as declines in insulin secretion and pancreatic beta-cell number, and to reduce monomeric eNAMPT-mediated increases in alpha-cell number in mouse islets. This mechanism highlights its potential therapeutic utility in the treatment of type 2 diabetes and other metabolic or inflammatory disorders.
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