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.
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- CAS No.: 3131794-81-2
- Formule: C26H25FN4O
- Masse moléculaire:428.50
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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
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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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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Masse moléculaire 428.50
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Formule 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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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)
BChE-IN-51 Related Classifications
HY-184664 Related Classifications
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