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

Tisolagiline methylsulfate  (Synonyms: KDS2010 methylsulfate)

Cat. No.: HY-127109A
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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 methylsulfate Chemical Structure

Tisolagiline methylsulfate Chemical Structure

CAS No. : 1894207-45-4

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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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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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Tisolagiline methylsulfate
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HY-127109A
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