AChE/MAO-B-IN-9
AChE/MAO-B-IN-9 (Compound E12) is an orally active, selective, reversible, non-competitive AChE and MAO-B inhibitor, with an IC50 of 0.156 μM against electric eel AChE. AChE/MAO-B-IN-9 inhibits Aβ40/42 fibril formation, promotes Aβ fibril depolymerization, and inhibits Tau protein fibril formation. AChE/MAO-B-IN-9 exerts antioxidant and neuroprotective effects, and improves scopolamine (HY-N0296)-induced memory impairment in mice. AChE/MAO-B-IN-9 can be used for the research of Alzheimer's disease.
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- CAS No.: 2341935-88-2
- 화학식: C21H20FN3O3
- 분자량:381.40
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보관:
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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
MAO-B |
EeAChE 0.156 μM (IC50) |
In Vitro
AChE/MAO-B-IN-9 (12 min) potently inhibits electric eel AChE with an IC50 of 0.156 ± 0.11 μM, and exhibits 36.79-fold higher selectivity for AChE over BuChE[1].
AChE/MAO-B-IN-9 (1 μM; 60 min) inhibits the activity of MAO-B in mouse liver mitochondria by 54.9 ± 2.7%[1].
AChE/MAO-B-IN-9 (0.625-10 μM; up to 80 h) inhibits Aβ40 fibril formation in a concentration-dependent manner, with an IC50 of 10.00 μM[1].
AChE/MAO-B-IN-9 (0.625-10 μM; up to 80 h) potently inhibits Aβ42 fibril formation in a concentration-dependent manner, with an IC50 of 1.01 μM[1].
AChE/MAO-B-IN-9 (2.5-10 μM; up to 50 h) inhibits Tau fibrillization with an IC50 of 4.50 μM, and reduces the plateau fluorescence intensity by 49% at a concentration of 10 μM[1].
AChE/MAO-B-IN-9 (1.25-20 μM; 24 h) inhibits Aβ secretion in SH-SY5Y cells in a concentration-dependent manner, and the inhibition rate of total Aβ reaches approximately 80% after treatment with 20 μM for 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cells
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Concentration:10-20 μM
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Incubation Time:24 h
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Result:Maintained cell viability within normal ranges (94-97%) when used alone.
Significantly counteracted Aβ40 and Aβ42 oligomer-induced toxicity, restoring cell survival toward control levels.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (male, 8 weeks old, SPF-grade)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Maintained stable body weights with minimal fluctuations relative to baseline.
Averaged 3.1 platform crossings at 1 mg/kg dose in Morris water maze test.
Averaged 3.9 platform crossings at 5 mg/kg dose in Morris water maze test.
Showed highly directed, efficient pathing toward the target quadrant on Day 5 at 5 mg/kg dose.
Caused no pathological alterations in heart, liver, spleen, lung, and kidney tissues.
Chemical Information
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CAS No. 2341935-88-2
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분자량 381.40
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화학식 C21H20FN3O3
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SMILES
O=C(C1=CC(C2=C(O1)C=CC(F)=C2)=O)NC3=CC=C(N4CCN(C)CC4)C=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AChE/MAO-B-IN-9 Related Classifications
HY-181861 Related Classifications
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