PZL-A
Based on 1 Customer Validation
PZL-A is a activator of mitochondrial DNA (mtDNA) synthesis. PZL-A restores wild-type-like activity to mutant forms of polymerase γ (POLγ) with AC50 s of 160 and 20 nM for A467T and G848S. PZL-A activates mtDNA synthesis in cells, enhancing biogenesis of the oxidative phosphorylation machinery and cellular respiration. PZL-A is promising for relieving POLG disease and other severe conditions linked to depletion of mtDNA.
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- Pureza: 99.72%
- No. CAS: 3068830-89-4
- Fòrmula: C19H17ClN4O2
- Peso molecular:368.82
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
PZL-A (0-100 μM, 10 min) dose-dependently activates the mutants (R232H, A467T, G848S, and W748S) (AC50: 20-200 nM), stabilizes the interaction with template, and interacts directly with the POLγ holoenzyme with increase of unfolding temperature[1].
PZL-A (1 μM, 0-15 min) stimulates DNA synthesis and enhances the rate of dNTP incorporation in mutants (R232H, A467T, G848S and W748S) without influence on exonuclease activity across a broad range of dNTP concentrations (0.08-10 µM)[1].
PZL-A (10 μM) interacting directly with the POLγ holoenzyme and increasing the unfolding temperature in mutants (R232H, A467T, G848S and W748S)[1].
PZL-A binds to a hydrophobic pocket between POLγA and POLγB with a C-shaped orientation, and the site is generally unaffected by most disease-causing mutations[1].
PZL-A (10 μM, 7.5-60 min) has a marked stimulatory effect, leading to DNA synthesis of longer double-stranded DNA (dsDNA) products [1].
PZL-A (1-3 μM, 7-14 days) strongly stimulates mtDNA repopulation rates with good tolerance in A467T/G848S and W748S/R232H mutant fibroblasts as well as quiescent fibroblasts[1].
PZL-A (0.00001-10 μM, 5-10 days) dose-dependently stimulates full-length mtDNA repopulation and increases 7S DNA levels in A467T/G848S and W748S/R232H mutant fibroblasts[1].
PZL-A (0.02-1 μM, 7-10 days) increases mtDNA levels and ameliorates OXPHOS activity in A467T/G848S and W748S/R232Hmutant fibroblasts and G848S/G848S mutant NSCs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 3068830-89-4
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Appearance Solid
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Peso molecular 368.82
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Fòrmula C19H17ClN4O2
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Color White to off-white
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SMILES
ClC1=CC=CC2=C1OCC[C@@H]2NC(NC3=NN(C4=CC=CC=C4)C=C3)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (271.13 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.
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.
Pureza y Documentación
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Ficha de datos (271 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.7113 mL | 13.5567 mL | 27.1135 mL | 67.7837 mL |
| 5 mM | 0.5423 mL | 2.7113 mL | 5.4227 mL | 13.5567 mL | |
| 10 mM | 0.2711 mL | 1.3557 mL | 2.7113 mL | 6.7784 mL | |
| 15 mM | 0.1808 mL | 0.9038 mL | 1.8076 mL | 4.5189 mL | |
| 20 mM | 0.1356 mL | 0.6778 mL | 1.3557 mL | 3.3892 mL | |
| 25 mM | 0.1085 mL | 0.5423 mL | 1.0845 mL | 2.7113 mL | |
| 30 mM | 0.0904 mL | 0.4519 mL | 0.9038 mL | 2.2595 mL | |
| 40 mM | 0.0678 mL | 0.3389 mL | 0.6778 mL | 1.6946 mL | |
| 50 mM | 0.0542 mL | 0.2711 mL | 0.5423 mL | 1.3557 mL | |
| 60 mM | 0.0452 mL | 0.2259 mL | 0.4519 mL | 1.1297 mL | |
| 80 mM | 0.0339 mL | 0.1695 mL | 0.3389 mL | 0.8473 mL | |
| 100 mM | 0.0271 mL | 0.1356 mL | 0.2711 mL | 0.6778 mL |
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