AChE/BChE-IN-37
AChE/BChE-IN-37 is a blood-brain barrier-permeable AChE/BChE inhibitor, with an IC50 of 73.65 μM against electric eel-derived AChE and an IC50 of 82.93 μM against horse-derived BChE. AChE/BChE-IN-37 exhibits chelating activity towards Cu2+, Ca2+, Mg2+, Fe2+ and Zn2+. AChE/BChE-IN-37 interacts with HSP90AA1 and GSK-3β. AChE/BChE-IN-37 inhibits the self-induced aggregation of Aβ1-42. AChE/BChE-IN-37 suppresses LPS-induced NO production in cells. AChE/BChE-IN-37 can be used in research related to Alzheimer's disease and inflammatory diseases.
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- Formule: C26H22F2N2O2
- Masse moléculaire:432.46
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
electric eel AChE 73.65 μM (IC50) |
equine serum BChE 82.93 μM (IC50) |
GSK-3β |
HSP90AA1 |
In Vitro
AChE/BChE-IN-37 (multiple concentration gradients; 15 min compound + enzyme, 10 min substrate addition) potently inhibits electric eel-derived AChE with an IC50 of 73.65 μM[1].
AChE/BChE-IN-37 (multiple concentration gradients; 15 min compound + enzyme, 10 min substrate addition) inhibits horse serum-derived BChE with an IC50 of 82.93 μM[1].
AChE/BChE-IN-37 (25 μM; 24 h) inhibits Aβ1-42 aggregation by 35.30% at a concentration of 25 μM[1].
AChE/BChE-IN-37 (25-200 μM; 24 h) shows no significant cytotoxicity in BV2 cells at concentrations up to 150 μM, with mild cytotoxicity observed at 200 μM[1].
AChE/BChE-IN-37 (25 μM; 3 h) exhibits chelating abilities with Cu2+, Ca2+, Mg2+, Fe2+, and Zn2+ ions[1].
AChE/BChE-IN-37 (25-200 μM; 24 h pre-incubation, 24 h LPS stimulation) potently inhibits LPS-induced NO production in BV2 cells with an IC50 of 31.42 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:BV2 microglial cells
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Concentration:25-200 μM
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Incubation Time:24 h
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Result:Showed no significant cytotoxicity at concentrations up to 150 μM, with BV2 cell survival rate greater than 85%.
Exhibited mild cytotoxicity at 200 μM, with cell survival rate around 80%.
Chemical Information
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Masse moléculaire 432.46
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Formule C26H22F2N2O2
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SMILES
O=C(C1=CC=C(N2CCN(C(C3=CC=C(F)C(F)=C3)=O)CC2)C=C1)/C=C/C4=CC=CC=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)