AChE-IN-24
AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD).
For research use only. We do not sell to patients.
- CAS No.: 3033542-32-1
- Formula: C22H30N2O4S2
- Molecular Weight:450.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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AChE |
In Vitro
AChE-IN-24 (compound 4c2) has good hAChE inhibitory activity with IC50values of 0.053 μM but owns little inhibition to hBuChE[1].
AChE-IN-2 has inhibitory activity for electric eel acetylcholinesterase (eeAChE) and equine serum butyrylcholinesterase (eqBuChE) with IC50values of 0.088 μM and 7.5μM, respectively[1].
AChE-IN-24 (0-0.2 μM) can cross the BBB comfortably by means of passive diffusion[1].
AChE-IN-2 (0-40 μM) triggers the translocation of Nrf2 to the nucleus, thereby expediting the binding of Nrf2 to the ARE for the transcription process[1].
AChE-IN-2 (7 μM) significantly induces the expression of antioxidant-related enzymes by activating Nrf2 in BV-2 cells[1].
AChE-IN-2 (1, 3, 7 μM) protects cells from H2O2-induced damage and inhibits ROS accumulation[1].
AChE-IN-2 (1, 3, 7 μM) attenuates inflammatory responses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:BV-2 microglial cells
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Concentration:0, 2.5, 5, 10, 20 and 40 μM
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Incubation Time:24 h
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Result:Not observed significant cytotoxicity.
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Cell Line:BV-2 microglial cells
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Concentration:7 μM
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Incubation Time:0-15 h
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Result:Up-regulated the amount of total Nrf2 in a time-dependent manner, decreased gradually the cytosolic Nrf2 level with its continuous accumulation in the nucleus and increased the total cellular Nrf2 accumulation in concentration-dependently.
Increased the protein expression levels of HO-1, NQO1, and GPX4 in a concentration-dependent manner with the biggest upregulation observed at 10 μM and significantly increased the protein levels of HO-1, NQO1, and GPX4 reaching the maximum at 9h, 6 h, and 3 h, respectively[1].
In Vivo
AChE-IN-24 (7.5 mg/kg, 15 mg/kg and 30mg/kg; once) ameliorates cognitive deficit induced by Scopolamine, suggesting a practicable therapeutic effect on AD[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KM mice[1]
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Dosage:0, 625, 1250, and 2500 mg/kg
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Administration:oral; 0, 625, 1250, and 2500 mg/kg
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Result:Not discovered abnormal behavior and acute toxicity were monitored for the first 4 h after administration, no acute neurological toxicities inclusive of tremor, convulsion, and death and no obvious signs of poisoning in the heart, liver, lungs, kidneys, and brain.
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Animal Model:The cognitive deficit mice model[1]
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Dosage:7.5 mg/kg, 15 mg/kg and 30mg/kg
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Administration:7.5 mg/kg, 15 mg/kg and 30mg/kg; once
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Result:Reversed the step-down latency and number of errors in a concentration-dependent manner.
Chemical Information
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CAS No. 3033542-32-1
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Molecular Weight 450.61
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Formula C22H30N2O4S2
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SMILES
O=C(OC)/C=C/C(NC1=CC=CC(OCCCCSC(N2C(C)CCCC2)=S)=C1)=O
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AChE-IN-24 Related Classifications
HY-151152 Related Classifications
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