AChE/BChE-IN-23
AChE/BChE-IN-23 (Compound 6e) is an AChE/BChE inhibitor (IC50: 0.91 μM, 1.19 μM and 1.01 μM for hAChE, eq BChE and hBChE, respectively). AChE/BChE-IN-23 has antioxidant activity and inhibits Aβ1-42 and Tau protein aggregation. AChE/BChE-IN-23 also inhibits microglial activation by reducing ROS release and mitochondrial injury. AChE/BChE-IN-23 suppresses NLRP3 inflammasome and pro-inflammatory cytokines in human microglial cells. AChE/BChE-IN-23 also reverses the Scopolamine (HY-N0296)-induced memory impairment in mice model.
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- Formel: C19H21N5O3
- Molecular Weight:367.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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hAChE 0.91 μM (IC50) |
eqBCHE 1.19 μM (IC50) |
NLRP3 |
hBCHE 1.02 μM (IC50) |
AChE/BChE-IN-23 (5-50 μM) causes propidium iodide (has a binding affinity for AChE enzyme) displacement from AChE (5 μM, 2.06%; 10 μM, 11.78%; 20 μM, 14.47%; 50 μM, 27.53%)[1].
AChE/BChE-IN-23 has antioxidant properties (20 μM; radical scavenging of DPPH: 47.30%, IC50:15.17 μM)[1].
AChE/BChE-IN-23 (3.125 μM, 72 h) effectively inhibits Aβ1-42 (12.5 μM) aggregation[1].
AChE/BChE-IN-23 (1.125 μM, 72 h) effectively inhibits Tau (5 μM) aggregation[1].
AChE/BChE-IN-23 (1-20 μM, 24 h) has no cytotoxicity effect on PC-12 cells[1]..
AChE/BChE-IN-23 (12.5 μM, 24 h) inhibits the activation of microglia by reducing the release of ROS and restoring the mitochondrial membrane potential[1].
AChE/BChE-IN-23 (12.5 μM, 24 h) has anti-inflammatory effect by inhibiting NLRP3 inflammasome and NF-κB expression levels in microglial cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HMC-3 cells
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Concentration:12.5 μM
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Incubation Time:24 h
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Result:Suppressed NLRP3, caspase-1, IL-1β and IL-18 expression.
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Cell Line:HMC-3 cells
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Concentration:12.5 μM
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Incubation Time:24 h
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Result:Reduced mitochondrial ROS and stabilizes the mitochondrial membrane potential.
AChE/BChE-IN-23 (2000 mg/kg, p.o., 14 days) has no toxicological effect on Swiss albino mice including no increase in overweight, abnormal behavior, convulsions, tremors, or diarrhea associated with acute toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Scopolamine (1 mg/kg) induced Alzheimer’s disease (AD) model; 6-week-old Swiss albino mice[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (i.p.), 14 days
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Result:Decreased escape latency, distance traveled in Morris Water Maze (MWM) experiment.
Increased latency period in passive avoidance.
Increased BDNF and Nr4a2 in brain.
Chemical Information
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Molecular Weight 367.40
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Formel C19H21N5O3
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SMILES
N/C(C1=CC=CC(NC(NCCC2=CNC3=C2C=C(OC)C=C3)=O)=C1)=N\O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AChE/BChE-IN-23 Related Classifications
HY-159898 Related Classifications
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