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CAS No. : 2237268-08-3
MCE 国际站:SBI-797812
产品活性: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。
研究领域:Metabolic Enzyme/Protease
作用靶点:NAMPT
In Vitro: 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.
In Vivo: SBI-797812 (10 mg/kg; i.p. or o.p.; single dose) shows high plasma exposure by intraperitoneal injection, with Cmax 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.
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