BuChE-IN-11
BuChE-IN-11 (Compound 3b-1) is an selective BuChE inhibitor with an IC50 of 0.44 μM for hBuChE. BuChE-IN-11 has high blood-brain barrier permeability and exhibits strong antioxidant activity due to its free radical scavenging properties. BuChE-IN-11 interacts with the choline binding site, acetyl binding site, and peripheral anionic site, exhibiting submicromolar BuChE inhibitory activity and preventing β-amyloid (Aβ) self-aggregation. BuChE-IN-11 holds promise for research in the field of Alzheimer's disease.
For research use only. We do not sell to patients.
- Formula: C28H27FN4O2
- Molecular Weight:470.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
hBCHE 0.44 μM (IC50) |
eqBCHE |
In Vitro
BuChE-IN-11 (Compound 3b-1) (0.1-1 µM, 120 min) demonstrates strong antioxidant activity[1]. BuChE-IN-11 (20 μM, 48h) inhibits the aggregation of αβ1-42[1]. BuChE-IN-11 (12.5-100 μM for PC12, 25-100 μM for AML12 over 24 hours) shows no significant toxicity to PC12 and AML12 cells at concentrations below 25 μM[1]. BuChE-IN-11 exhibits good blood-brain barrier permeability (CNS+) after 18 hours, indicating its ability to cross the blood-brain barrier[1]. BuChE-IN-11 is predicted to have high gastrointestinal absorption activity and low risk of cardiac toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:PC12 and AML12 cells
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Concentration:12.5-100 μM for PC12, 25-100 μM for AML12
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Incubation Time:24 h
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Result:Only exhibited significant cytotoxicity at concentrations greater than 25 µM. At concentrations below 25 µM, BuChE-IN-11 shows no significant cytotoxicity against PC12 and AML12 cells.
Chemical Information
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Molecular Weight 470.54
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Formula C28H27FN4O2
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SMILES
O=C(NCCC1=CNC2=C1C=CC=C2)[C@@H](NCC3=CC=C(O)C(F)=C3)CC4=CNC5=C4C=CC=C5
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
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Amyloid: Congo Red Amyloid Staining
Congo red amyloid staining is a histochemical method used to detect extracellular amyloid deposits in tissue sections based on the affinity of Congo red dye for β-pleated sheet-rich protein aggregates. When bound to amyloid, Congo red produces characteristic apple-green birefringence under polarized light microscopy, which is widely regarded as a diagnostic feature of amyloid deposition in histopathology. The diagnostic principle relies on the combination of dye binding (congophilia) and optical anisotropy under polarized illumination, which distinguishes amyloid from most non-amyloid eosinophilic extracellular deposits in routine histological evaluation. Amyloid identification by Congo red staining remains a cornerstone in diagnostic pathology despite the availability of adjunct methods such as immunohistochemistry and mass spectrometry, particularly because of its ability to localize deposits directly within tissue architecture. The specificity of Congo red-positive deposits is incre
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)