Gardell, Stephen J.; Hopf, Meghan; Khan, Asima; Dispagna, Mauro; Hampton Sessions, E.; Falter, Rebecca; Kapoor, Nidhi; Brooks, Jeanne; Culver, Jeffrey; Petucci, Chris; Ma, Chen-Ting; Cohen, Steven E.; Tanaka, Jun; Burgos, Emmanuel S.; Hirschi, Jennifer S.; Smith, Steven R.; Sergienko, Eduard; Pinkerton, Anthony B. published the artcile< Boosting NAD+ with a small molecule that activates NAMPT>, Formula: C6H8N2, the main research area is lung carcinoma cell NAMPT SBI797812 NAD.
Pharmacol. strategies that boost intracellular NAD+ are highly coveted for their therapeutic potential. One approach is activation of nicotinamide phosphoribosyltransferase (NAMPT) to increase production of NMN (NMN), the predominant NAD+ precursor in mammalian cells. A high-throughput screen for NAMPT activators and hit-to-lead campaign yielded SBI-797812, a compound that is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT. SBI-797812 shifts the NAMPT reaction equilibrium towards NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT at His247, promotes consumption of the pyrophosphate byproduct, and blunts feedback inhibition by NAD+. These effects of SBI-797812 turn NAMPT into a “”super catalyst”” that more efficiently generates NMN. Treatment of cultured cells with SBI-797812 increases intracellular NMN and NAD+. Dosing of mice with SBI-797812 elevates liver NAD+. Small mol. NAMPT activators such as SBI-797812 are a pioneering approach to raise intracellular NAD+ and realize its associated salutary effects.
Nature Communications published new progress about Biomarkers. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Formula: C6H8N2.