1. Neuronal Signaling
  2. Cholinesterase (ChE) Monoamine Oxidase Amyloid-β Tau Protein
  3. 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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AChE/MAO-B-IN-9

AChE/MAO-B-IN-9 Chemical Structure

CAS No. : 2341935-88-2

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Description

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[1].

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.

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 10-20 μM
Incubation Time: 24 h
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

AChE/MAO-B-IN-9 (1-5 mg/kg; p.o.; daily; 7 days) dose-dependently improves Scopolamine (HY-N0296) -induced spatial memory deficits in male ICR mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mice (male, 8 weeks old, SPF-grade)[1]
Dosage: 1 mg/kg; 5 mg/kg
Administration: p.o.; daily; 7 days
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.
Molecular Weight

381.40

Formula

C21H20FN3O3

CAS No.
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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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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    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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AChE/MAO-B-IN-9
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HY-181861
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