1. Neuronal Signaling
  2. Monoamine Oxidase
  3. Tisolagiline monomethylsulfate

Tisolagiline monomethylsulfate  (Synonyms: KDS2010 monomethylsulfate)

Cat. No.: HY-127109A Purity: 99.83% ee.: 100.00%
Handling Instructions Technical Support

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.

Tisolagiline monomethylsulfate

Tisolagiline monomethylsulfate Chemical Structure

CAS No. : 1894207-45-4

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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target[1]

MAO-B

8 nM (IC50)

In Vitro

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.

Immunofluorescence[2]

Cell Line: Human astrocytes
Concentration: 1 μM
Incubation Time: 4 days
Result: Inhibited the expression of GFAP.
In Vivo

Tisolagiline methylsulfate (10 mg/kg, po, once daily for 30 days) ameliorates MPTP (HY-15608)-induced Parkinson’s disease in mouse models[1].
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.

Animal Model: MPTP-induced Parkinson’s disease in mouse models[1]
Dosage: 10 mg/kg
Administration: po, once daily for 30 days
Result: Alleviated the motor dysfunction, reversed the reduction in the number of TH-positive neurons, reduced the expression of GFAP and iNOS.
Animal Model: U87 MG xenograft mouse models[2]
Dosage: 10 mg/kg
Administration: po for 1-7 days
Result: Increased the fluorescence signal of DOX in the GBM area, increased the volume of GBM tumors.
Molecular Weight

418.43

Formula

C18H21F3N2O4S

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3899 mL 11.9494 mL 23.8989 mL
5 mM 0.4780 mL 2.3899 mL 4.7798 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Tisolagiline monomethylsulfate
Cat. No.:
HY-127109A
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