2. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. NAMPT ATP Synthase
  4. NAMPT activator-10

NAMPT activator-10 (Compound B11) 是一种具有口服活性的 NAMPT 激活剂，其靶标 Kd 值为 0.64 μM。NAMPT activator-10 可激活 NAD+ 生物合成过程中的限速酶，促进细胞内 NAD+ 的合成。NAMPT activator-10 可减少乳酸堆积、增强肝脏与肌肉的糖原储存、提升组织 ATP 生成、改善运动耐力与肌肉力量，并在小鼠疲劳模型中对疲劳诱导的肌肉损伤具有保护作用。NAMPT activator-10 可用于肌肉疲劳相关研究。

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NAMPT activator-10

NAMPT activator-10 Chemical Structure

CAS No. : 2237269-22-4

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NAMPT activator-10 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NAMPT activator-10 (Compound B11) is an orally active NAMPT activator with a target Kd value of 0.64 μM. NAMPT activator-10 activates the rate-limiting enzyme in NAD+ biosynthesis and promotes intracellular NAD+ synthesis. NAMPT activator-10 reduces lactate accumulation, enhances glycogen storage in the liver and muscle, increases tissue ATP production, improves exercise endurance and muscle strength, and exerts a protective effect against fatigue-induced muscle damage in mouse fatigue models. NAMPT activator-10 can be used in studies related to muscle fatigue[1].

体外研究
(In Vitro)

NAMPT activator-10 (0-8.0 μM) 可浓度依赖性地强效激活纯化的 NAMPT 酶，最大激活效应达 206%[1]。
NAMPT activator-10 (0-5.00 μM) 以高亲和力 (Kd = 0.64 μM) 结合纯化的 NAMPT 酶[1]。
NAMPT activator-10 (0-4.0 μM; 4 h) 可在 4 小时内浓度依赖性地升高 THLE-2 肝细胞内的 NAD+ 水平[1]。
NAMPT activator-10 (72 h) 在 THLE-2 肝细胞 (IC50 = 316 μM) 和 C2C12 小鼠肌管细胞 (IC50 = 236 μM) 中处理 72 h 后显示出低细胞毒性[1]。
NAMPT activator-10 (1.25-10.0 μM) 可浓度依赖性地提高 C2C12 小鼠肌管中 AMPK 的磷酸化水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NAMPT activator-10 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ Bioavailability
Mice[1] 2 mg/kg i.v. 0.969 h 0.083 h 491 ng/mL 209 212 /
Mice[1] 20 mg/kg p.o. 3 h 1.5 h 75.3 ng/mL 209 233 11 %
Mice[1] 10 mg/kg i.p. 5.15 h 0.25 h 119 ng/mL 521 539 50.9 %
体内研究
(In Vivo)

NAMPT activator-10 (20 mg/kg；腹腔注射；每日一次；连续 3 天) 可通过减少乳酸堆积并提升肝脏与肌肉组织中的能量储备来缓解小鼠肌肉疲劳[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (male, 7-week-old, 19−23 g, muscle fatigue model via daily treadmill running for 1 h over 6 consecutive days)[1]
Dosage: 20 mg/kg
Administration: i.p.; daily; 3 days
Result: Reduced serum lactate levels significantly.
Increased serum lactate dehydrogenase content.
Increased hepatic glycogen stores 3.1-fold compared to controls.
Increased muscle glycogen stores 1.5-fold compared to controls.
Animal Model: C57BL/6J (male, 7-week-old, 19−23 g, muscle fatigue-induced muscle damage model via treadmill running)[1]
Dosage: 20 mg/kg
Administration: i.p.; daily; 3 days
Result: Preserved skeletal muscle ultrastructure with well-ordered myofibrils, reduced sarcoplasmic vacuolization, increased mitochondrial size and number, and intact mitochondrial cristae compared to the fatigue model group.
Increased skeletal muscle NAD+ levels 1.5-fold compared to controls.
Increased skeletal muscle ATP levels 1.8-fold compared to controls.
Increased NAD+ and ATP levels significantly in heart, liver, and kidney tissues.
Detected no pathological abnormalities in major organs.
分子量

412.46

Formula

C20H20N4O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NAMPT activator-10 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NAMPT activator-102237269-22-4NAMPT activator10NAMPT activator 10NAMPTATP SynthaseNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factormuscle cellsNAD+A549THLE-2 human liver cellsHEK-293TC2C12 mouse myotubesC2C12 cellsmouse fatigue modelsAMPKInhibitorinhibitorinhibit

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