Minzasolmin
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Minzasolmin (UCB0599; (R)-NPT200-11) is an orally active, blood-brain-permeable α-synuclein (α-Syn) inhibitor that selectively binds to α-Syn misfolded intermediates (such as oligomers) and inhibits aggregation and fibril formation by regulating their conformational stability. Minzasolmin can reduce the generation of pathological oligomers and block neurotoxic signaling, thereby reducing the abnormal accumulation of α-Syn in the brain. Minzasolmin significantly improved motor deficits, reduced neuroinflammatory markers, and α-Syn-related pathological deposition in transgenic mouse models.
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- Pureza: 98.60%
- No. CAS: 1802518-92-8
- Fòrmula: C23H31N5OS
- Peso molecular:425.59
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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
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α-synuclein Aggregation |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Thy1-αSyn transgenic mice[1]
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Dosage:1 mg/kg or 5 mg/kg, dissolved in DMSO/saline
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Administration:Intraperitoneal (IP) injection, daily (Monday to Friday), 3-month treatment period
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Result:Significantly improved motor coordination (rotarod latency increased by 20% in 5 mg/kg group) and reduced gait abnormalities compared to vehicle controls.
Western blot analysis showed a dose-dependent decrease in insoluble α-synuclein (α-Syn) aggregates in the cortex and hippocampus (50% reduction at 5 mg/kg), accompanied by downregulation of neuroinflammatory markers (IL-6, TNF-α) and normalization of striatal dopamine transporter (DAT) levels.
Immunohistochemistry revealed fewer phosphorylated α-Syn (p-Ser129) positive inclusions in substantia nigra neurons, indicating attenuation of α-Syn pathology and neuroinflammation.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1802518-92-8
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Appearance Solid
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Peso molecular 425.59
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Fòrmula C23H31N5OS
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Color Off-white to light yellow
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SMILES
O=C(C1=CN=C(N2CCN(CC2)C)S1)N[C@H](CCCC)CC3=CNC4=CC=CC=C34
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Synonyms
UCB0599; (R)-NPT200-11
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvente y solubilidad
DMSO : 100 mg/mL (234.97 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)
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 (5.87 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 (5.87 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 (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.
Pureza y Documentación
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Ficha de datos (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)
- Portuguese - PT (252 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 (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 | 2.3497 mL | 11.7484 mL | 23.4968 mL | 58.7420 mL |
| 5 mM | 0.4699 mL | 2.3497 mL | 4.6994 mL | 11.7484 mL | |
| 10 mM | 0.2350 mL | 1.1748 mL | 2.3497 mL | 5.8742 mL | |
| 15 mM | 0.1566 mL | 0.7832 mL | 1.5665 mL | 3.9161 mL | |
| 20 mM | 0.1175 mL | 0.5874 mL | 1.1748 mL | 2.9371 mL | |
| 25 mM | 0.0940 mL | 0.4699 mL | 0.9399 mL | 2.3497 mL | |
| 30 mM | 0.0783 mL | 0.3916 mL | 0.7832 mL | 1.9581 mL | |
| 40 mM | 0.0587 mL | 0.2937 mL | 0.5874 mL | 1.4685 mL | |
| 50 mM | 0.0470 mL | 0.2350 mL | 0.4699 mL | 1.1748 mL | |
| 60 mM | 0.0392 mL | 0.1958 mL | 0.3916 mL | 0.9790 mL | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2937 mL | 0.7343 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2350 mL | 0.5874 mL |
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