SBI-797812 | NAMPT activator

NAMPT is the rate-limiting enzyme in the nicotinamide adenine dinucleotide (NAD⁺) salvage pathway that converts nicotinamide to nicotinamide mononucleotide (NMN) which is responsible for most of the NAD⁺ formation in mammals.¹ Cellular levels of NAD⁺ have been shown to decrease with age and NAMPT is believed to be a key enzyme in the aging/senescence process.² SBI-797812 (2237268-08-3) is a NAMPT activator, turning it into a “super catalyst” that more efficiently generates NMN.³ It increases NMN levels and prevents NAD⁺ feedback inhibition in a cell-free assay using recombinant human NAMPT at a concentration of 2 µM. In mice (20 mg/kg), it increases liver levels of NAD⁺ and shows a trend toward increased levels in cardiac tissue but does not affect levels in the quadriceps, or gastrocnemius.³

References/Citations:

1. Revollo et al. (2007), The regulation of nicotinamide adenine dinucleotide biosynthesis by Nampt/PBEF/visfatin in mammals; Curr. Opin. Gastroenterol., 23 164
2. Khaidizar et al. (2021), Nicotinamide Phosphoribosyltransferase as a Key Molecule of the Aging/Senescence Process; Int. J. Mol. Sci., 22 3709
3. Gardell et al. (2019), Boosting NAD⁺ with a small molecule that activates NAMPT; Nat. Commun., 10 3241