2. Neuronal Signaling Immunology/Inflammation MAPK/ERK Pathway
  3. Cholinesterase (ChE) Toll-like Receptor (TLR) p38 MAPK Interleukin Related Complement System
  4. 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.

For research use only. We do not sell to patients.

BuChE-IN-23

BuChE-IN-23 Chemical Structure

CAS No. : 3067571-93-8

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BuChE-IN-23 Related Antibodies

Top Publications Citing Use of Products

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AChE BChE

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

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[1].
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.

BuChE-IN-23 Related Antibodies

Cell Viability Assay[1]

Cell Line: mouse microglial BV2 cells
Concentration: 20 μM
Incubation Time: 24 h
Result: Maintained cell viability above 90% at 20 μM, indicating acceptable cytocompatibility.
In Vivo

BuChE-IN-23 (Compound E14) (3-10 mg/kg; p.o.; daily; 14 days) significantly improves recognition memory and spatial learning performance, and suppresses oAβ-induced hippocampal glial activation and neuroinflammation in male C57BL/6 J mice with oligomeric Aβ-induced cognitive impairment[1].
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.

Animal Model: C57BL/6 J (male, 3 months old, intracerebroventricular injection of oligomeric Aβ1-42 on Day 1 and Day 7)[1]
Dosage: 3 mg/kg; 10 mg/kg
Administration: p.o.; daily; 14 days
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.
Molecular Weight

435.47

Formula

C25H25NO6
CAS No.
SMILES

O=C1C(OCC2=CC=CC=C2)=C(/C=C/C3=CC=C(O)C=C3)OC(COC(N(CC)C)=O)=C1
Shipping

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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BuChE-IN-23 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

BuChE-IN-233067571-93-8Cholinesterase (ChE)Toll-like Receptor (TLR)p38 MAPKInterleukin RelatedComplement SystemILnitric oxideIL-1β/C3-mediated microglia-astrocyte inflammatory axislipopolysaccharidealzheimer's diseaseacetylcholinesterasehippocampal glial activationneuroinflammationTLR4/p38 MAPK signalingBV2 microglial cellsbutyrylcholinesteraseInhibitorinhibitorinhibit

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