Nampt activator-4
Based on 1 Customer Validation
Nampt activator-4 is an orally active NAMPT activator, with an EC50 of 58 nM and a Ka of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD+, thereby enhancing enzymatic activity and significantly increasing intracellular NAD+ levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders.
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- Pureté: 98.87%
- CAS No.: 2847156-05-0
- Formule: C26H22F3N7OS
- Masse moléculaire:537.56
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
EC50: 0.058 μM (NAMPT)[1].
Nampt activator-4 (Compound 63) allosterically activates recombinant human NAMPT, with an EC50 of 58 nM and a Kd of 85.38 nM[1].
Nampt activator-4 (Compound 63) (0.001-10 μM; 24 h) increases NAD+ levels in THP-1 human leukemia monocytic cells, with an EC50 of 85 nM, and reaches approximately 140% of the control level after 24 h of treatment at 10 μM[1].
Nampt activator-4 (3 μM; 24 h) competes with the NAMPT inhibitor FK866 for binding to NAMPT in human leukemia monocytic cells THP-1, and reduces the inhibitory potency of FK866[1].
Nampt activator-4 is rapidly metabolized in mouse and human liver microsomes, with half-lives of 2.3 min and 4.2 min, respectively[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/6 mice (male, 20-40 g)[1]
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Dosage:30 mg/kg
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Administration:p.o.; single dose
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Result:Achieved a maximal plasma concentration of 3.2 μM.
Reached a plasma concentration of 180 nM at 3 h post-administration.
Chemical Information
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CAS No. 2847156-05-0
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Appearance Solid
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Masse moléculaire 537.56
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Formule C26H22F3N7OS
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Color White to off-white
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SMILES
O=C([C@@H]1CN(CCN1)C2=NC=NC3=NN(C=C32)C4=CC=C(C=C4)C(F)(F)F)NCC5=CC=C6SC=CC6=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (186.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8603 mL | 9.3013 mL | 18.6026 mL | 46.5064 mL |
| 5 mM | 0.3721 mL | 1.8603 mL | 3.7205 mL | 9.3013 mL | |
| 10 mM | 0.1860 mL | 0.9301 mL | 1.8603 mL | 4.6506 mL | |
| 15 mM | 0.1240 mL | 0.6201 mL | 1.2402 mL | 3.1004 mL | |
| 20 mM | 0.0930 mL | 0.4651 mL | 0.9301 mL | 2.3253 mL | |
| 25 mM | 0.0744 mL | 0.3721 mL | 0.7441 mL | 1.8603 mL | |
| 30 mM | 0.0620 mL | 0.3100 mL | 0.6201 mL | 1.5502 mL | |
| 40 mM | 0.0465 mL | 0.2325 mL | 0.4651 mL | 1.1627 mL | |
| 50 mM | 0.0372 mL | 0.1860 mL | 0.3721 mL | 0.9301 mL | |
| 60 mM | 0.0310 mL | 0.1550 mL | 0.3100 mL | 0.7751 mL | |
| 80 mM | 0.0233 mL | 0.1163 mL | 0.2325 mL | 0.5813 mL | |
| 100 mM | 0.0186 mL | 0.0930 mL | 0.1860 mL | 0.4651 mL |
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