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

NAMPT activator-10 Chemical Structure

CAS No. : 2237269-22-4

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NAMPT activator-10 Related Antibodies

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Description

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].

In Vitro

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.

NAMPT activator-10 Related Antibodies
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 %
In Vivo

Compound B11 (20 mg/kg; i.p.; daily; 3 days) alleviates muscle fatigue by reducing lactate buildup and increasing energy reserves in liver and muscle tissue[1].

MedChemExpress (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.
Molecular Weight

412.46

Formula

C20H20N4O4S
CAS No.
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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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NAMPT activator-10 Related Classifications

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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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