BuChE-IN-23
BuChE-IN-23 is an orally active, blood-brain barrier permeable butyrylcholinesterase (eqBuChE) inhibitor with an IC50 of 15.59 μM and a Ki of 29.33 μM. BuChE-IN-23 exhibits an IC50 of 38.65 μM against hBuChE and shows selectivity for butyrylcholinesterase over acetylcholinesterase. BuChE-IN-23 inhibits LPS (HY-D1056)-induced nitric oxide production, attenuates hippocampal glial cell activation and neuroinflammation, suppresses the TLR4/p38 MAPK signaling pathway, and regulates the IL-1β/C3-mediated microglia-astrocyte inflammatory axis. BuChE-IN-23 can be used for the research of Alzheimer's disease.
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- CAS No.: 3067571-93-8
- Formule: C25H25NO6
- Masse moléculaire:435.47
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
eqBCHE 15.59 μM (IC50) |
BuChE 38.65 μM (IC50) |
IL-1β |
In Vitro
BuChE-IN-23 (Compound E14) (20 μM; 24 h) exhibits extremely low cytotoxicity in BV2 microglial cells[1].
BuChE-IN-23 (15 μM; 25 h) potently inhibits lipopolysaccharide-induced nitric oxide production in BV2 microglia, with an IC50 of 9.76 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse microglial BV2 cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:Maintained cell viability above 90% at 20 μM, indicating acceptable cytocompatibility.
In Vivo
BuChE-IN-23 (500 mg/kg; p.o.; single dose) exhibits good acute tolerability in mice, with no observable organ toxicity following a single oral dose of 500 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 J (male, 3 months old, intracerebroventricular injection of oligomeric Aβ1-42 on Day 1 and Day 7)[1]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Significantly increased the discrimination ratio relative to the oAβ group, comparable to Rivastigmine.
Markedly increased the number of platform crossings relative to the oAβ group, comparable to Rivastigmine.
Significantly reduced hippocampal IBA1 and 6E10 fluorescence intensity, attenuating microglial activation and Aβ deposition.
Significantly downregulated hippocampal protein levels of IBA1, GFAP, TLR4, and IL-1β, and reduced the p-p38/p38 ratio relative to the oAβ group.
Significantly reduced hippocampal GFAP and TNF-α fluorescence intensity, suppressing astrocytic activation and pro-inflammatory cytokine expression.
Significantly decreased hippocampal IL-1β and C3 fluorescence intensity, attenuating microglial IL-1β production and astrocytic C3 activation.
Chemical Information
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CAS No. 3067571-93-8
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Masse moléculaire 435.47
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Formule C25H25NO6
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SMILES
O=C1C(OCC2=CC=CC=C2)=C(/C=C/C3=CC=C(O)C=C3)OC(COC(N(CC)C)=O)=C1
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BuChE-IN-23 Related Classifications
HY-183352 Related Classifications
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Keywords
- BuChE-IN-23
- 3067571-93-8
- Cholinesterase (ChE)
- Toll-like Receptor (TLR)
- p38 MAPK
- Interleukin Related
- Complement System
- nitric oxide
- IL-1β/C3-mediated microglia-astrocyte inflammatory axis
- lipopolysaccharide
- alzheimer's disease
- acetylcholinesterase
- hippocampal glial activation
- neuroinflammation
- TLR4/p38 MAPK signaling
- BV2 microglial cells
- butyrylcholinesterase
- Inhibitor
- inhibitor
- inhibit