NAMPT activator-10
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.
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- CAS No.: 2237269-22-4
- Formula: C20H20N4O4S
- Molecular Weight:412.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
NAMPT activator-10 (0-8.0 μM) potently activates purified NAMPT enzyme in a concentration-dependent manner, with a maximum activation effect reaching 206%[1].
NAMPT activator-10 (0-5.00 μM) binds to purified NAMPT enzyme with high affinity (Kd = 0.64 μM)[1].
NAMPT activator-10 (0-4.0 μM; 4 h) increases intracellular NAD+ levels in THLE-2 hepatocytes in a concentration-dependent manner within 4 hours[1].
NAMPT activator-10 (72 h) exhibits low cytotoxicity after 72 h of treatment in THLE-2 hepatocytes (IC50 = 316 μM) and C2C12 mouse myotube cells (IC50 = 236 μM)[1].
NAMPT activator-10 (1.25-10.0 μM) increases the phosphorylation level of AMPK in C2C12 mouse myotubes in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 3 days
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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.
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Animal Model:C57BL/6J (male, 7-week-old, 19−23 g, muscle fatigue-induced muscle damage model via treadmill running)[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 3 days
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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.
Chemical Information
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CAS No. 2237269-22-4
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Molecular Weight 412.46
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Formula C20H20N4O4S
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SMILES
O=C(NC1=CC=C(C=C1)NS(=O)(C2=CC=C(C=C2)OC)=O)NCC3=CC=NC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)