SBI-797812

SBI-797812 is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT with EC50 of 0.37 μM. 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 by-product, and blunts feedback inhibition by NAD+. Treatment of cultured cells with SBI-797812 increases intracellular NMN and NAD+. Dosing of mice with SBI-797812 elevates liver NAD+[1].

Research Areas >> Metabolic Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Nampt

NAMPT[1]

[1]. Gardell SJ , et al. Boosting NAD+ with a small molecule that activates NAMPT. Nat Commun. 2019 Jul 19;10(1):3241.