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。

SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD in mice.

Solid

NAMPT

SBI-797812 (0-4 μM; 4 h) activates NAMPT in a dose-dependent manner with an EC50 value of 0.37 μM, and (1 μM, 2 μM; 1 h) increases NAMPT-mediated NMN in cells.
SBI-797812 (2 μM; 1 or 4 h) exerts NAMPT (30 nM) activation requiring ATP (2 mM).
SBI-797812 (5 μM; 2 h) impacts PP (20 μM) consumption and pHisNAMPT reactivity.
SBI-797812 (0.4, 2, 10 μM; 4 h) increases the level of nicotinamide mononucleotide (NMN) and NAD in A549 human lung carcinoma cells as well as in human or mouse primary myotubes at 10 μM.
SBI-797812, as an NRAMPT activator plays a role in successive aging promotion, while NAMPT is a rate limiting enzyme in NAD salvage pathway of Aging/Senescence process.
has not independently confirmed the accuracy of these methods. They are for reference only.

SBI-797812 (10 mg/kg; i.p. or o.p.; single dose) shows high plasma exposure by intraperitoneal injection, with C max value of 3297?ng/mL, 8.2?μM.
SBI-797812 (20 mg/kg; i.p.; single dose; measured 2?h post-dose) significant increases NAD in mouse liver.
has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. Gardell SJ , et al. Boosting NAD+ with a small molecule that activates NAMPT. Nat Commun. 2019 Jul 19;10(1):3241.
[2]. Khaidizar FD, et al. Nicotinamide Phosphoribosyltransferase as a Key Molecule of the Aging/Senescence Process. Int J Mol Sci. 2021 Apr 2;22(7):3709. 

In Vitro: DMSO : 250 mg/mL (621.16 mM; Need ultrasonic)配制储备液