GNE-8505
Based on 1 Customer Validation
GNE-8505 is an orally active, blood-brain barrier-permeable selective dual leucine zipper kinase (DLK) inhibitor. GNE-8505 has an IC50 of 0.144 μM for pJNK, and EC50 of 0.457 μM for DRG. GNE-8505 inhibits the DLK/JNK pathway, reduces stress-induced c-Jun phosphorylation levels, decreases neuronal death and suppresses axonal degeneration. GNE-8505 reduces phosphorylated c-Jun levels in the retina, spinal cord and brain tissues of mice. GNE-8505 is applicable to research related to Alzheimer's disease and amyotrophic lateral sclerosis (ALS).
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- Pureza: 99.53%
- No. CAS: 1620573-48-9
- Fòrmula: C21H24F3N5O
- Peso molecular:419.44
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
Single administration of GNE-8505 (35 mg/kg) significantly reduces the number of phosphorylated c-Jun-positive cells in the spinal cord of SOD1G93A ALS mice at the middle stage of the disease[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N (SOD1G93A transgenic line, 14-week-old, mid-disease stage)[2]
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Dosage:35 mg/kg
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Administration:single dose
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Result:Reduced the number of p-c-Jun-positive cells in lumbar spinal cord sections compared to vehicle-treated mice.
Chemical Information
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No. CAS 1620573-48-9
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Appearance Solid
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Peso molecular 419.44
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Fòrmula C21H24F3N5O
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Color White to off-white
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SMILES
FC(F)(F)C1=CC(C2=NN(C([C@@H]3[C@]4([H])[C@@]3([H])CN(C5COC5)C4)=C2)CC6CC6)=CN=C1N
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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 (238.41 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)
Pureza y Documentación
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Ficha de datos (273 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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Instrucciones de manejo (2659 KB)
Referencias
[2]. Le Pichon CE, et al. Loss of dual leucine zipper kinase signaling is protective in animal models of neurodegenerative disease. Sci Transl Med. 2017;9(403):eaag0394. [Content Brief]
[3]. Siu M, et al. JW. Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. J Med Chem. 2018 Sep 27;61(18):8078-8087. [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, 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 | 2.3841 mL | 11.9207 mL | 23.8413 mL | 59.6033 mL |
| 5 mM | 0.4768 mL | 2.3841 mL | 4.7683 mL | 11.9207 mL | |
| 10 mM | 0.2384 mL | 1.1921 mL | 2.3841 mL | 5.9603 mL | |
| 15 mM | 0.1589 mL | 0.7947 mL | 1.5894 mL | 3.9736 mL | |
| 20 mM | 0.1192 mL | 0.5960 mL | 1.1921 mL | 2.9802 mL | |
| 25 mM | 0.0954 mL | 0.4768 mL | 0.9537 mL | 2.3841 mL | |
| 30 mM | 0.0795 mL | 0.3974 mL | 0.7947 mL | 1.9868 mL | |
| 40 mM | 0.0596 mL | 0.2980 mL | 0.5960 mL | 1.4901 mL | |
| 50 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1921 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3974 mL | 0.9934 mL | |
| 80 mM | 0.0298 mL | 0.1490 mL | 0.2980 mL | 0.7450 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5960 mL |
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