Tisolagiline monomethylsulfate
Based on 1 Customer Validation
Tisolagiline methylsulfate (KDS2010) is the selective, reversible and orally active inhibitor for MAO-B with an IC50 of 8 nM. Tisolagiline methylsulfate exhibits neuroprotective and anti-neuroinflammatory activities.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 1894207-45-4
- Formula: C18H21F3N2O4S
- Molecular Weight:418.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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MAO-B 8 nM (IC50) |
Tisolagiline methylsulfate (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 methylsulfate (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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CAS No. 1894207-45-4
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Appearance Solid
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Molecular Weight 418.43
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Formula C18H21F3N2O4S
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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.CS(=O)(O)=O
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Synonyms
KDS2010 monomethylsulfate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 20 mg/mL (47.80 mM; ultrasonic and adjust pH to 2 with 1 M HCl; 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)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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. 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 | 2.3899 mL | 11.9494 mL | 23.8989 mL | 59.7472 mL |
| 5 mM | 0.4780 mL | 2.3899 mL | 4.7798 mL | 11.9494 mL | |
| 10 mM | 0.2390 mL | 1.1949 mL | 2.3899 mL | 5.9747 mL | |
| 15 mM | 0.1593 mL | 0.7966 mL | 1.5933 mL | 3.9831 mL | |
| 20 mM | 0.1195 mL | 0.5975 mL | 1.1949 mL | 2.9874 mL | |
| 25 mM | 0.0956 mL | 0.4780 mL | 0.9560 mL | 2.3899 mL | |
| 30 mM | 0.0797 mL | 0.3983 mL | 0.7966 mL | 1.9916 mL | |
| 40 mM | 0.0597 mL | 0.2987 mL | 0.5975 mL | 1.4937 mL |