AMPK activator 18
Based on 1 Customer Validation
AMPK activator 18 is a potent allosteric activator of AMPK complexes containing the β2 isoform. AMPK activator 18activates α2-containing AMPK α2β2γ1 and α2β2γ3 complexes, with EC50 values of 17.2 and 82.1 nM. AMPK activator 18 stimulates β2-AMPK in cells, and glucose uptake by isolated skeletal muscle. AMPK activator 18 induces acetyl-coenzyme A carboxylase (ACC) and AMPK α-T172 phosphorylation. AMPK activator 18 can be used for the research of type 2 diabetes.
For research use only. We do not sell to patients.
- CAS No.: 1364692-88-5
- Formula: C26H18ClN3O4
- Molecular Weight:471.90
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All AMPK Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
AMPK α2β2γ1 17.2 nM (EC50) |
α2β2γ3 82.1 nM (EC50) |
In Vitro
AMPK activator 18 potently and selectively activates α2-containing AMPK complexes, particularly the skeletal muscle-enriched α2β2γ1 and α2β2γ3 complexes, with EC50 values of 17.2 ± 1.6 nM and 82.1 ± 1.3 nM respectively, and its activation is dependent on the β2-D111 residue but not the β2 N-terminal helix[1].
AMPK activator 18 (0.03-10 μM; 1 h) triggers AMPK signaling in differentiated C2C12 myotubes and β2-reconstituted iMEFs via an allosteric mechanism independent of changes to intracellular AMP/ATP ratio or AMPK α-T172 phosphorylation, inducing dose-dependent ACC phosphorylation[1].
AMPK activator 18 (1-2 μM) increases ACC phosphorylation and AMPK α-T172 phosphorylation levels in Epitrochlearis muscles[1].
AMPK activator 18 (10 μM) reduces 2-deoxyglucose (2DG) uptake in soleus and extensor digitorum longus muscles[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:β2-expressing b1/2 dKO iMEFs
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Concentration:1 μM; 10 μM
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Incubation Time:1 h
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Result:Induced a significant increase in ACC phosphorylation without altering AMPK α-T172 phosphorylation in β2-reconstituted iMEFs at 1 μM.
Induced ACC phosphorylation associated with an increase in AMPK α-T172 phosphorylation in β2-reconstituted iMEFs at 10 μM.
Chemical Information
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CAS No. 1364692-88-5
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Appearance Solid
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Molecular Weight 471.90
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Formula C26H18ClN3O4
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Color White to off-white
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SMILES
O=C(O)C1=CC(OC2=NC3=NC(=C(Cl)C=C3N2)C4=CC=C(C=C4)C5=CC=CC=C5O)=CC=C1C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
In Vitro:
DMSO : 10 mg/mL (21.19 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
In Vivo:
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: ≥ 1 mg/mL (2.12 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.12 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 (stored under nitrogen). 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 | 2.1191 mL | 10.5955 mL | 21.1909 mL | 52.9773 mL |
| 5 mM | 0.4238 mL | 2.1191 mL | 4.2382 mL | 10.5955 mL | |
| 10 mM | 0.2119 mL | 1.0595 mL | 2.1191 mL | 5.2977 mL | |
| 15 mM | 0.1413 mL | 0.7064 mL | 1.4127 mL | 3.5318 mL | |
| 20 mM | 0.1060 mL | 0.5298 mL | 1.0595 mL | 2.6489 mL |
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