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).
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- CAS No.: 3033542-32-1
- Formule: C22H30N2O4S2
- Masse moléculaire:450.61
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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
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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.
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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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Masse moléculaire 450.61
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Formule 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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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)
AChE-IN-24 Related Classifications
HY-151152 Related Classifications
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