AJ-4
AJ-4 is an orally active, blood-brain barrier-permeable GSK-3β/AChE inhibitor, with an IC50 of 4.7 nM against GSK-3β and 2.97 μM against AChE. AJ-4 increases the level of phosphorylated GSK-3β and reduces the expression of Amyloid-β and phosphorylated Tau. AJ-4 improves scopolamine-induced learning and memory impairment and alleviates hippocampal neuron damage in AD mice. AJ-4 can be used for the research of Alzheimer's disease.
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- Formule: C23H21Cl3N4O5S
- Masse moléculaire:571.86
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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GSK-3β 4.7 nM (IC50) |
AChE 2.97 μM (IC50) |
AJ-4 (10 μM; 24 h) significantly restores the viability of SH-SY5Y cells damaged by Aβ25-35[1].
AJ-4 (5-20 μM; 24 h) regulates key Alzheimer's disease (AD)-related proteins in Aβ25-35-damaged SH-SY5Y cells in a concentration-dependent manner, with the specific mechanism involving upregulation of p-GSK-3β and downregulation of APP and p-Tau[1].
AJ-4 (5-20 μM; 24 h) concentration-dependently inhibits Aβ25-35-induced secretion of TNF-α and IL-1β in SH-SY5Y cells, exhibiting anti-inflammatory activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Aβ25-35-injured SH-SY5Y human neuroblastoma cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Restored cell viability from 54.3% (Aβ25-35-injured level) to 98.98%.
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Cell Line:Aβ25-35-stimulated SH-SY5Y human neuroblastoma cells
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Concentration:5, 10, 20 μM
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Incubation Time:24 h
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Result:Concentration-dependently reduced Aβ25-35-upregulated TNF-α and IL-1β levels.
Showed the highest reduction of pro-inflammatory cytokines at 20 μM.
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Cell Line:Aβ25-35-injured SH-SY5Y human neuroblastoma cells
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Concentration:5, 10, 20 μM
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Incubation Time:24 h
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Result:Concentration-dependently downregulated APP and phosphorylated Tau (p-Tau) levels relative to the Aβ25-35-injured model group.
Concentration-dependently upregulated phosphorylated GSK-3β (p-GSK-3β) levels relative to the Aβ25-35-injured model group.
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, scopolamine-induced AD-like behavior)[1]
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Dosage:0.5 mg/kg; 1.0 mg/kg; 2.0 mg/kg
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Administration:p.o.; daily; 18 days
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Result:Reduced orientation navigation escape latency in a dose-dependent manner starting from day 3 of training.
Increased the number of virtual platform crossings relative to the model group at 0.5 mg/kg.
Increased both the percentage of movement distance in the target quadrant and the number of virtual platform crossings relative to the model group at 1.0 mg/kg and 2.0 mg/kg.
Significantly downregulated APP and phosphorylated Tau (p-Tau) expression, while significantly upregulated phosphorylated GSK-3β (p-GSK-3β) expression relative to the model group at all tested doses.
Preserved clear hippocampal histomorphology, with only slight neuronal pyknosis and hyperchromasia limited to CA1 and DG regions at 1.0 mg/kg and 2.0 mg/kg.
Resulted in intact hippocampal structure with only sporadic pyknotic neurons in the CA3 region at 2.0 mg/kg.
Chemical Information
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Masse moléculaire 571.86
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Formule C23H21Cl3N4O5S
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SMILES
C=CC(NC1=C(C=CC(N2SC(N(C2=O)CC3=CC=C(C=C3)OC(N(CCCl)CCCl)=O)=O)=C1)Cl)=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)
AJ-4 Related Classifications
HY-184742 Related Classifications
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