SBI-797812 是一种在结构上类似于活性位点定向的 NAMPT 抑制剂的化合物，可以阻断这些抑制剂与 NAMPT 的结合，EC50 为 0.37 μM。 SBI-797812 将 NAMPT 反应平衡转向 NMN 形成，增加 NAMPT 对 ATP 的亲和力，稳定 His247 处的磷酸化 NAMPT，促进焦磷酸盐副产物的消耗，并通过 NAD+ 钝化反馈抑制。 用 SBI-797812 处理培养的细胞可增加细胞内 NMN 和 NAD+。 用 SBI-797812 在小鼠中可提高肝脏 NAD+。
CAS：2237268-08-3
分子式：C19H22N4O4S
分子量：402.47
纯度：98%
存储：Store at -20°C

Background:

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]. NAMPT[1]

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