Tisolagiline
Based on 1 Customer Validation
Tisolagiline (KDS2010) is the selective, reversible and orally active inhibitor for MAO-B with an IC50 of 8 nM. Tisolagiline exhibits neuroprotective and anti-neuroinflammatory activities.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.85%
- No. CAS: 1894207-44-3
- Fòrmula: C17H17F3N2O
- Peso molecular:322.32
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Almacenamiento:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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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Orally Active Compound Library
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Neuroprotective Compound Library
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Anti-Parkinson's Disease Compound Library
HY-L085
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Neurodegenerative Disease-related Compound Library
HY-L086
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Mitochondria-Targeted Compound Library
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Antidepressant Compound Library
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Metabolic Enzyme Compound Library
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Highly Selective Inhibitors Library
HY-L158
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HY-L001
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Actividad biológica
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MAO-B 8 nM (IC50) |
Tisolagiline (1 μM, 4 days) reduces the expression of glial fibrillary acidic protein (GFAP) and the deposition of glycosaminoglycans (CSPGs), thereby inhibiting the astrocyte activation and the astrocyte scar formation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human astrocytes
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Concentration:1 μM
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Incubation Time:4 days
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Result:Inhibited the expression of GFAP.
Tisolagiline (10 mg/kg/day, po for 1-7 days) inhibits astrocyte scar formation, thereby increasing the penetration of Doxorubicin (HY-15142) into glioblastoma domain, increases the volume of GBM tumor in mouse models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MPTP-induced Parkinson’s disease in mouse models[1]
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Dosage:10 mg/kg
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Administration:po, once daily for 30 days
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Result:Alleviated the motor dysfunction, reversed the reduction in the number of TH-positive neurons, reduced the expression of GFAP and iNOS.
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Animal Model:U87 MG xenograft mouse models[2]
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Dosage:10 mg/kg
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Administration:po for 1-7 days
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Result:Increased the fluorescence signal of DOX in the GBM area, increased the volume of GBM tumors.
Chemical Information
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No. CAS 1894207-44-3
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Appearance Solid
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Peso molecular 322.32
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Fòrmula C17H17F3N2O
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Color White to off-white
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SMILES
C[C@H](NCC1=CC=C(C2=CC=C(C(F)(F)F)C=C2)C=C1)C(N)=O
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Synonyms
KDS2010
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 100 mg/mL (310.25 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 (protect from light). 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 (protect from light). 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Nam MH, et al. KDS2010, a Newly Developed Reversible MAO-B Inhibitor, as an Effective Therapeutic Candidate for Parkinson's Disease. Neurotherapeutics. 2021 Jul;18(3):1729-1747. [Content Brief]
[2]. Diep YN, et al., Astrocytic scar restricting glioblastoma via glutamate-MAO-B activity in glioblastoma-microglia assembloid. Biomater Res. 2023 Jul 19;27(1):71 [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 (protect from light). 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 | 3.1025 mL | 15.5125 mL | 31.0251 mL | 77.5627 mL |
| 5 mM | 0.6205 mL | 3.1025 mL | 6.2050 mL | 15.5125 mL | |
| 10 mM | 0.3103 mL | 1.5513 mL | 3.1025 mL | 7.7563 mL | |
| 15 mM | 0.2068 mL | 1.0342 mL | 2.0683 mL | 5.1708 mL | |
| 20 mM | 0.1551 mL | 0.7756 mL | 1.5513 mL | 3.8781 mL | |
| 25 mM | 0.1241 mL | 0.6205 mL | 1.2410 mL | 3.1025 mL | |
| 30 mM | 0.1034 mL | 0.5171 mL | 1.0342 mL | 2.5854 mL | |
| 40 mM | 0.0776 mL | 0.3878 mL | 0.7756 mL | 1.9391 mL | |
| 50 mM | 0.0621 mL | 0.3103 mL | 0.6205 mL | 1.5513 mL | |
| 60 mM | 0.0517 mL | 0.2585 mL | 0.5171 mL | 1.2927 mL | |
| 80 mM | 0.0388 mL | 0.1939 mL | 0.3878 mL | 0.9695 mL | |
| 100 mM | 0.0310 mL | 0.1551 mL | 0.3103 mL | 0.7756 mL |
Tisolagiline Related Classifications
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