SBI-797812是一种有效的烟酰胺磷酸核糖基转移酶 (NAMPT) 激活剂,能增加细胞内 NMN 和 NAD+ 水平,改善能量代谢。它对提高细胞能量状态和改善代谢疾病具有潜在的研究价值。
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产品名称 | NAMPT ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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CHS-828 |
+++
NAMPT, IC50: <25 nM NAMPT, Kd: 120 nM |
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STF-118804 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | SBI-797812 functions as an orally active activator of nicotinamide phosphoribosyltransferase (NAMPT). It induces a shift in NAMPT activity towards NMN formation, enhances NAMPT's affinity for ATP, stabilizes phosphorylated NAMPT, facilitates the consumption of pyrophosphate by-product, and attenuates feedback inhibition by NAD+. SBI-797812 leads to elevated intracellular nicotinamide mononucleotide (NMN) levels and increased liver NAD+ concentrations in mice[1][2]. |
体内研究 | SBI-797812 (10 mg/kg; i.p. or o.p.; single dose) exhibits substantial plasma exposure following intraperitoneal administration, with Cmax value of 3297 ng/mL, 8.2 μM[1]. SBI-797812 (20 mg/kg; i.p.; single dose; measured 2 h post-dose) markedly elevates NAD+ levels in mouse liver[1]. |
体外研究 | SBI-797812 (0-4 μM; 4 h) dose-dependently stimulates NAMPT activation, exhibiting an EC50 value of 0.37 μM, and (1 μM, 2 μM; 1 h) enhances NAMPT-mediated NMN production in cells[1]. SBI-797812 (2 μM; 1 or 4 h) induces activation of NAMPT (30 nM), dependent on ATP (2 mM) availability[1]. SBI-797812 (5 μM; 2 h) influences PP (20 μM) utilization and the reactivity of pHisNAMPT[1]. SBI-797812 (0.4, 2, 10 μM; 4 h) elevates the concentration of nicotinamide mononucleotide (NMN) and NAD+ in A549 human lung carcinoma cells, as well as in human or mouse primary myotubes at 10 μM[1]. SBI-797812, functioning as an NRAMPT activator, contributes to the progression of aging. NAMPT serves as a rate-limiting enzyme in the NAD+ salvage pathway of the aging/senescence process[2]. |
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存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.48mL 0.50mL 0.25mL |
12.42mL 2.48mL 1.24mL |
24.85mL 4.97mL 2.48mL |
CAS号 | 2237268-08-3 |
分子式 | C19H22N4O4S |
分子量 | 402.467 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 250 mg/mL(621.17 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |