SBI-797812 是一种口服有效的烟酰胺磷酸核糖基转移酶 (NAMPT) 激活剂。SBI-797812 激活 NAMPT 向 NMN 转变，增加 NAMPT 对 ATP 的亲和力，稳定磷酸化 NAMPT，促进焦磷酸盐副产物的消耗，并减弱 NAD+ 的反馈抑制。SBI-797812 增加细胞内 NMN，并提高小鼠肝脏内 NAD+ 水平。 Information SBI-797812 SBI-797812 is a NAMPT activator which is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT . SBI-797812 turns NAMPT into a "super catalyst" that more efficiently generates NMN. Targets NAMPT In vitro 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+. In vivo Plasma concentrations of SBI-797812 after oral administration are low. Higher plasma levels of SBI-797812 are seen after i.p. dosing. The potency of SBI-797812 against mouse NAMPT is investigated. The apparent affinity (EC50) of SBI-797812 for mouse NAMPT is approximately 8-fold less than for human NAMPT, whereas maximal fold activation by SBI-797812 is comparable between the mouse and human NAMPT. Dosing of mice with SBI-797812 elevates liver NAD+. Cell Research(from reference) Cell lines：Human A549 lung carcinoma cells Concentrations：10 μM Incubation Time：4 h