Multi-target kinase-IN-10
Multi-target kinase-IN-10 (Compound 6l) is an orally active, blood-brain barrier-permeable, selective, reversible, and competitive MAO-B inhibitor with an IC50 of 0.0053 μM. Multi-target kinase-IN-10 competes with substrates for binding to the active site of MAO-B, chelates Cu2+ ions, inhibits Cu2+-induced ROS production, and reduces the release of NO, TNF-α, and IL-1β. Multi-target kinase-IN-10 ameliorates Parkinson's disease.
For research use only. We do not sell to patients.
- CAS No.: 3022330-81-7
- Formula: C17H13FN2O2
- Molecular Weight:296.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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IL-1β |
MAO-B 0.0053 μM (IC50) |
Multi-target kinase-IN-10 potently and selectively inhibits MAO-B with an IC50 of 0.0053 μM and a selectivity index greater than 1904.7[1].
Multi-target kinase-IN-10 (0.5-10.0 μM) dose-dependently inhibits LPS-induced release of NO, TNF-α and IL-1β in BV-2 microglia[1].
Multi-target kinase-IN-10 (2.5-10.0 μM) dose-dependently inhibits LPS-induced ROS production in BV-2 microglia, with inhibition rates of 18.9% and 41.7% at concentrations of 2.5 μM and 10.0 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-stimulated
BV-2 cells -
Concentration:0.5-10.0 μM
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Incubation Time:Unclear
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Result:Exhibited potent TNF-α suppression, with inhibition rates
of 35.0%, 56.4%, and 82.1% at 0.5, 2.5, 10.0 μM, respectively.
Exhibited IL-1β suppression, with inhibition rates
of 37.5%, 54.5%, and 75.2% at 0.5, 2.5, 10.0 μM, respectively.
| Species | Dose | Route | Cmax | Tmax (Plasma) | T1/2 | AUC0-t | Tmax (Brain) |
|---|---|---|---|---|---|---|---|
| Mice[1] | 37.5 mg/kg | p.o. | 1177.55 (plasma) ng/mL | 1.0 (plasma) h | 1.96 (plasma) h | 3522.34 (plasma) μg/L·h | 1.0 (brain) h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (10 per group, MPTP-induced subacute model)[1]
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Dosage:7.5 mg/kg; 15 mg/kg; 37.5 mg/kg
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Administration:i.g.; daily
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Result:Significantly reduced motor deficits across all behavioral tests on days 1, 3, 7, and 14 at 37.5 mg/kg compared to the model group.
Showed significant improvements in most behavioral measures by day 7 at 15 mg/kg compared to the model group.
Showed a decreasing trend in motor deficits by day 3 and significant improvements by day 7 at 7.5 mg/kg compared to the model group.
Increased striatal dopamine levels by 60.5% at 37.5 mg/kg compared to the model group.
Reduced striatal malondialdehyde (MDA) content by 53.6% at 37.5 mg/kg compared to the model group.
Inhibited striatal TNF-α release by 67.1% and IL-6 release by 72.7% at 37.5 mg/kg relative to the model group.
Moderately restored dopamine levels, inhibited TNF-α release by 48.9%, and IL-6 release by 62.1% at 15 mg/kg compared to the model group.
Showed moderate dopamine recovery, inhibited TNF-α release by 24.2%, and IL-6 release by 45.8% at 7.5 mg/kg compared to the model group.
Significantly increased tyrosine hydroxylase (TH)-positive cell count in the substantia nigra pars compacta and enhanced TH-immunoreactive fiber density in the striatum at 37.5 mg/kg compared to the model group.
Chemical Information
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CAS No. 3022330-81-7
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Molecular Weight 296.30
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Formula C17H13FN2O2
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SMILES
OC1=CC=CC=C1C2=NN=C(OCC3=CC=C(F)C=C3)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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