ZLN024 hydrochloride
Based on 1 publication(s) in Google Scholar
ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.51%
- CAS. Nr.: 1883548-91-1
- Formel: C13H14BrClN2OS
- Molecular Weight:361.69
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
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Publications Citing Use of MedChemExpress (MCE) ZLN024 hydrochloride
MoreAlle AMPK Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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AMPK α2β2γ1 0.13 μM (EC50) |
AMPK α1β1γ1 0.42 μM (EC50) |
AMPK α2β1γ1 0.95 μM (EC50) |
ZLN024 allosterically stimulates active AMPK heterotrimers and the inactive α1 subunit truncations α1 (1-394) and α1 (1-335) but not α1 (1-312). AMPK activation by ZLN024 requires the pre-phosphorylation of Thr-172 by at least one upstream kinase and protects AMPK Thr-172 against dephosphorylation by PP2Cα. ZLN024 activates AMPK in L6 myotubes and stimulates glucose uptake and fatty acid oxidation without increasing the ADP/ATP ratio. Using the established scintillation proximity assay (SPA) assay, random screening against the AMPK α1β1γ1 heterotrimer is performed and a new AMPK activator, ZLN024 is found. ZLN024 directly activates recombinant AMPK α1β1γ1 and its homologue α2β1γ1 in a concentration-dependent manner. ZLN024 increases the activity of α1β1γ1 by 1.5-fold and has an EC50 of 0.42 µM, and it increases the activity of α2β1γ1 by 1.7-fold with an EC50 of 0.95 µM. ZLN024 also directly activates recombinant AMPK α1β2γ1, by 1.7-fold with an EC50 of 1.1 µM; and AMPK α2β2γ1, by 1.6-fold with an EC50 of 0.13 µM[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.
Chemical Information
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CAS. Nr. 1883548-91-1
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Appearance Solid
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Molecular Weight 361.69
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Formel C13H14BrClN2OS
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Color White to off-white
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SMILES
CC1=CC=C(OCCSC2=NC=CC=N2)C(Br)=C1.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
Circadian rhythm modulates endochondral bone formation via MTR1/AMPKβ1/BMAL1 signaling axis. [Abstract]2022 Apr;29(4):874-887. PMID: 35094018
Lösungsmittel & Löslichkeit
DMSO : ≥ 46 mg/mL (127.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (6.91 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.91 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 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protokoll
Before the scintillation proximity assay (SPA) assay, 200 nM recombinant AMPK protein (α1β1γ1, α2β1γ1, α1β2γ1, α2β2γ1, α1(1-394), α1(1-335), α1(1-312)) is constructed, expressed, purified and fully phosphorylated. The SPA reactions are performed in 96-well plates in a final volume of 50 µL containing 20 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM DTT, 2 µM biotin-SAMS, 2 µM ATP and 7.4×103 Bq/well [γ-33P]ATP. The reactions are initiated by the addition of 50 nM recombinant AMPK protein to the reaction solutions, followed by incubation at 30°C for 2 hr. The reactions are then terminated by the addition of 40 µL of stop solution containing 80 µg Streptavidin-coated SPA beads per well, 50 mM EDTA and 0.1% Triton X-100 in PBS, pH 7.5, followed by incubation for 1 hr. Finally, 160 µL of suspension solution containing 2.4 M CsCl, 50 mM EDTA and 0.1% Triton X-100 in PBS, pH 7.5, is added to the reaction solution to suspend the SPA beads completely. The SPA signals are measured in a Wallac Microbeta plate counter 30 min later[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
C57BKS db/db mice are maintained under a 12 hr light-dark cycle with free access to water and food. At 8 weeks of age, male db/db mice are randomly assigned to the various treatment groups by body weight and glucose levels (n=6-8). The treatment groups for the 5-week chronic study are as follows: vehicle (0.5% methylcellulose), ZLN024 (15 mg/kg) and Metformin (250 mg/kg). The treatments are orally administered once daily. The body weights and food intake are measured daily. After 5 weeks of treatment, the mice are killed after a final dose, and the tissues are collected for further analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (286 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)
Verweise
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 (sealed storage, away from moisture). 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 | 2.7648 mL | 13.8240 mL | 27.6480 mL | 69.1200 mL |
| 5 mM | 0.5530 mL | 2.7648 mL | 5.5296 mL | 13.8240 mL | |
| 10 mM | 0.2765 mL | 1.3824 mL | 2.7648 mL | 6.9120 mL | |
| 15 mM | 0.1843 mL | 0.9216 mL | 1.8432 mL | 4.6080 mL | |
| 20 mM | 0.1382 mL | 0.6912 mL | 1.3824 mL | 3.4560 mL | |
| 25 mM | 0.1106 mL | 0.5530 mL | 1.1059 mL | 2.7648 mL | |
| 30 mM | 0.0922 mL | 0.4608 mL | 0.9216 mL | 2.3040 mL | |
| 40 mM | 0.0691 mL | 0.3456 mL | 0.6912 mL | 1.7280 mL | |
| 50 mM | 0.0553 mL | 0.2765 mL | 0.5530 mL | 1.3824 mL | |
| 60 mM | 0.0461 mL | 0.2304 mL | 0.4608 mL | 1.1520 mL | |
| 80 mM | 0.0346 mL | 0.1728 mL | 0.3456 mL | 0.8640 mL | |
| 100 mM | 0.0276 mL | 0.1382 mL | 0.2765 mL | 0.6912 mL |
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