BChE-IN-51
BChE-IN-51 is a selective, blood-brain barrier-permeable, orally active BChE inhibitor with an IC50 of 0.03 μM against hBChE. BChE-IN-51 reduces ROS production, protects neurons from the toxic effects of hydrogen peroxide and Aβ1-42, and alleviates cognitive impairment. BChE-IN-51 can be used for the research of Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 3131794-81-2
- Formula: C26H25FN4O
- Molecular Weight:428.50
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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 0.03 μM (IC50) |
In Vitro
BChE-IN-51 (Compound W13) (1 nM-100 μM; 5 min) potently and selectively inhibits butyrylcholinesterase (hBChE) with an IC50 of 0.03 μM, and shows extremely low activity against acetylcholinesterase (AChE)[1].
BChE-IN-51 (0-0.125 μM; 4 min) acts as a mixed-type inhibitor of hBChE, with a Ki of 0.57 μM, an α value of 17.3, and a Ki' of 9.9 μM[1].
BChE-IN-51 (1-100 μM; 24 h) exhibits low in vitro cytotoxicity against HT22, BV2 and SH-SY5Y cells, and maintains >90% cell viability at concentrations up to 20 μM after 24 h of incubation[1].
BChE-IN-51 (1-10 μM; 2 h) dose-dependently protects BV2 and SH-SY5Y cells against H2O2-induced damage, with the maximum protective effect observed at 10 μM[1].
BChE-IN-51 (1-10 μM; 2 h) dose-dependently protects SH-SY5Y cells from Aβ1-42-induced damage, and fully restores cell viability at concentrations of 5 and 10 μM[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:HT22 mouse hippocampal neuronal cells, BV2 mouse microglial cells, SH-SY5Y human neuroblastoma cells
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Concentration:1, 5, 10, 20, 50, 100 μM
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Incubation Time:24 h
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Result:Maintained cell survival above 90% across all three cell lines at concentrations up to 20 μM.
Induced cytotoxicity only at concentrations ≥50 μM.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming mice (male, 15−18 g, intracerebroventricular injection of Aβ1-42 oligopeptides to induce cognitive impairment)[1]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 12 days
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Result:Significantly shortened the escape latency to the target platform compared to the Aβ1-42 model group.
Reduced the swimming distance to the platform compared to the Aβ1-42 model group.
Restored cognitive function to near normal levels comparable to the positive control tacrine.
Showed no significant effect on mouse body weight during the experimental period.
Chemical Information
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CAS No. 3131794-81-2
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Molecular Weight 428.50
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Formula C26H25FN4O
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SMILES
FC1=CC=CC=C1C(N/C(NC2=CC=CC=C2CC)=N/CCC3=CNC4=C3C=CC=C4)=O
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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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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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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)