SBI-797812
Based on 2 publication(s) in Google Scholar
SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD+ in mice.
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- Purity: 99.88%
- CAS No.: 2237268-08-3
- 화학식: C19H22N4O4S
- 분자량:402.47
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SBI-797812
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Biological Activity
NAMPT[1]
SBI-797812 (0-4 μM; 4 h) activates NAMPT in a dose-dependent manner with an EC50 value of 0.37 μM, and (1 μM, 2 μM; 1 h) increases NAMPT-mediated NMN in cells[1].
SBI-797812 (2 μM; 1 or 4 h) exerts NAMPT (30 nM) activation requiring ATP (2 mM)[1].
SBI-797812 (5 μM; 2 h) impacts PP (20 μM) consumption and pHisNAMPT reactivity[1].
SBI-797812 (0.4, 2, 10 μM; 4 h) increases the level 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, as an NRAMPT activator plays a role in successive aging promotion, while NAMPT is a rate limiting enzyme in NAD+ salvage pathway of Aging/Senescence process[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SBI-797812 (20 mg/kg; i.p.; single dose; measured 2 h post-dose) significant increases NAD+ in mouse liver[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 J mice (8-week-old)[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection; administrated 1 h after fasting; added Buthanasia-D (165 mg/kg; i.p.) 4 h after fasting
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Result:Showed 0.311, 0.144, 0.078, and 0.078 μg/mg dry powder about NAD+ in liver, heart, gastrocnemius and quadriceps, respectively by LC-MS/MS measurement.
Chemical Information
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CAS No. 2237268-08-3
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Appearance Solid
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분자량 402.47
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화학식 C19H22N4O4S
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Color Light yellow to yellow
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SMILES
O=C(NCC1=CC=NC=C1)NC2=CC=C(S(=O)(N3CC(O4)CCC4C3)=O)C=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
용액&용해도
DMSO : 250 mg/mL (621.16 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: 2.08 mg/mL (5.17 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.08 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Gardell SJ , et al. Boosting NAD+ with a small molecule that activates NAMPT. Nat Commun. 2019 Jul 19;10(1):3241. [Content Brief]
[2]. Khaidizar FD, et al. Nicotinamide Phosphoribosyltransferase as a Key Molecule of the Aging/Senescence Process. Int J Mol Sci. 2021 Apr 2;22(7):3709. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4847 mL | 12.4233 mL | 24.8466 mL | 62.1164 mL |
| 5 mM | 0.4969 mL | 2.4847 mL | 4.9693 mL | 12.4233 mL | |
| 10 mM | 0.2485 mL | 1.2423 mL | 2.4847 mL | 6.2116 mL | |
| 15 mM | 0.1656 mL | 0.8282 mL | 1.6564 mL | 4.1411 mL | |
| 20 mM | 0.1242 mL | 0.6212 mL | 1.2423 mL | 3.1058 mL | |
| 25 mM | 0.0994 mL | 0.4969 mL | 0.9939 mL | 2.4847 mL | |
| 30 mM | 0.0828 mL | 0.4141 mL | 0.8282 mL | 2.0705 mL | |
| 40 mM | 0.0621 mL | 0.3106 mL | 0.6212 mL | 1.5529 mL | |
| 50 mM | 0.0497 mL | 0.2485 mL | 0.4969 mL | 1.2423 mL | |
| 60 mM | 0.0414 mL | 0.2071 mL | 0.4141 mL | 1.0353 mL | |
| 80 mM | 0.0311 mL | 0.1553 mL | 0.3106 mL | 0.7765 mL | |
| 100 mM | 0.0248 mL | 0.1242 mL | 0.2485 mL | 0.6212 mL |
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