BChE-IN-57
BChE-IN-57 is a mixed-type, selective BChE inhibitor with IC50 values of 0.20 and 0.35 μM for eqBChE and hBChE, respectively. BChE-IN-57 reduces hydrogen peroxide-induced intracellular ROS accumulation and mitochondrial membrane potential loss through antioxidant protection. BChE-IN-57 inhibits the production of NO and pro-inflammatory cytokines and downregulates inflammatory enzyme markers. BChE-IN-57 chelates metal ions, including copper. BChE-IN-57 can be used for research on Alzheimer's disease.
For research use only. We do not sell to patients.
- Formula: C25H23FN4O
- Molecular Weight:414.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
eqBCHE 0.20 μM (IC50) |
hBCHE 0.35 μM (IC50) |
eel AChE >50 μM (IC50) |
In Vitro
BChE-IN-57 (100-400 nM; 20 min) inhibits eqBChE in a mixed-type manner with a Ki of 0.112 µM[1].
BChE-IN-57 (6.25-100 µM) exhibits a favorable safety profile in HT22, BV2, and L02 cells, showing certain toxicity only at 50 and 100 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT22 cells
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Concentration:non-toxic concentrations (1.25-10 μM)
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Incubation Time:4 h (pre-incubation); 12 h (H2O2 exposure)
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Result:Improved the viability of H2O2-exposed cells to varying degrees.
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Cell Line:BV2 microglial cells
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Concentration:5, 10, 20 µM
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Incubation Time:4 h (pre-incubation)
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Result:LPS challenge significantly upregulated iNOS and COX-2.
At 20 µM, significantly downregulated both iNOS and COX-2 expression compared with the LPS-challenged group.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | MRT0-t |
|---|---|---|---|---|---|---|---|
| Mice[1] | 40 mg/kg | p.o. | 4.09 h | 1.33 h | 215.01 ng/mL | 958.38 ng·h/mL | 4.18 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Healthy C57BL mice[1]
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Dosage:1000 mg/kg
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Administration:p.o.
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Result:Showed that the physiological state of the mice is normal, as evidenced by stable food and water intake and continuous body weight gain.
No obvious abnormal behaviors or other clinical signs were observed.
- Mitochondrial membrane-potential fluorescent assay
- LPS-Induced Endotoxemia/Systemic Inflammation
- ROS/oxidative-stress fluorescent staining
- Fluorescent plasma-membrane potential dye assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Research Protocol for Inflammation-related Diseases
- Alzheimer’s Disease Modeling
Chemical Information
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Molecular Weight 414.47
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Formula C25H23FN4O
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SMILES
O=C(C1=CC(C2=NC=CC=C2)=NC3=CC=CC=C13)NCCN(CC4=CC=C(F)C=C4)C
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)