MTX115325
Based on 1 Customer Validation
MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine.
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- Pureza: 99.91%
- No. CAS: 2750895-97-5
- Fòrmula: C18H16N6O2
- Peso molecular:348.36
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Actividad biológica
IC50: 12 nM (USP30)
EC50: 32 nM (TOM20, the outer mitochondrial membrane protein)[1]
MTX115325 (37 nM-1 μM; 72 h) shows promotion of mitochondrial autophagy in SH-SY5Y cells[1].
MTX115325 (10 nM-1 μM; 90 min) promotes ubiquitination of TOM20 and inhibits USP30 activity in both HeLa cells and YFP-Parkin overexpressing HeLa cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MTX115325 (i.g.; 10 mg/kg; single dose) demonstrates excellent oral bioavailability (98%) and good CNS penetration with a brain partition coefficient (Kpu,u) of approximately 0.4[1].
MTX115325 (i.g.; single dose) has a Cmax of 7546.9 ng/mL at 15 mg/kg and a Cmax of 16374.3 ng/mL at 50 mg/kg. At a 50 mg/kg dosage, the drug concentration consistently remained above the EC50 for TOM20 ubiquitination[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AAV-A53T-SNCA Mouse Model [1]
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Dosage:15 mg/kg and 50 mg/kg
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Administration:i.g.; twice daily for 10 weeks
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Result:Reduced the loss of dopaminergic neurons in the substantia nigra (SN) and preserved dopamine levels in the striatum.
Increased the percentage of tyrosine hydroxylase (TH)+ neurons.
Chemical Information
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No. CAS 2750895-97-5
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Appearance Solid
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Peso molecular 348.36
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Fòrmula C18H16N6O2
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Color White to off-white
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SMILES
O=C(C1=NC=C(C2=CC=NC(C#N)=C2)O1)N3[C@]4([H])[C@@](CC3)([H])[C@H](N(C4)C#N)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 250 mg/mL (717.65 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)
- 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 | 2.8706 mL | 14.3530 mL | 28.7059 mL | 71.7648 mL |
| 5 mM | 0.5741 mL | 2.8706 mL | 5.7412 mL | 14.3530 mL | |
| 10 mM | 0.2871 mL | 1.4353 mL | 2.8706 mL | 7.1765 mL | |
| 15 mM | 0.1914 mL | 0.9569 mL | 1.9137 mL | 4.7843 mL | |
| 20 mM | 0.1435 mL | 0.7176 mL | 1.4353 mL | 3.5882 mL | |
| 25 mM | 0.1148 mL | 0.5741 mL | 1.1482 mL | 2.8706 mL | |
| 30 mM | 0.0957 mL | 0.4784 mL | 0.9569 mL | 2.3922 mL | |
| 40 mM | 0.0718 mL | 0.3588 mL | 0.7176 mL | 1.7941 mL | |
| 50 mM | 0.0574 mL | 0.2871 mL | 0.5741 mL | 1.4353 mL | |
| 60 mM | 0.0478 mL | 0.2392 mL | 0.4784 mL | 1.1961 mL | |
| 80 mM | 0.0359 mL | 0.1794 mL | 0.3588 mL | 0.8971 mL | |
| 100 mM | 0.0287 mL | 0.1435 mL | 0.2871 mL | 0.7176 mL |
MTX115325 Related Classifications
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