hAChE/hBACE-1-IN-4
hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research.
For research use only. We do not sell to patients.
- CAS No.: 229476-71-5
- Formula: C21H24N4O2
- Molecular Weight:364.44
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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hAChE 0.283 μM (IC50) |
hBCHE 0.231 μM (IC50) |
hAChE/hBACE-1-IN-4 (10, 20, 40 and 80 μM; 24 h) has non-neurotoxic properties[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y
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Concentration:10, 20, 40 and 80 μM
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Incubation Time:24 h
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Result:Reduced cell viability by 26% at maximum concentration (80 μM).
hAChE/hBACE-1-IN-4 (20 mg/kg; po, 9 days) inhibits ACE-1 activity to restore cognitive deficits and acts as an anti-Aβ agent at its tested doses in Wistar rats[1].
hAChE/hBACE-1-IN-4 (10 and 20 mg/kg; ig, 4 days) possesses the ability to cross the BBB and reaches their specific site of action in the brain[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats [1]
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Dosage:500 mg/kg for 14 days
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Administration:Oral gavage (p.o.)
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Result:Observed the renal and hepatic functional parameters within the prescribed limits
. Examined and found with normal tissue appearance such as kidneys, heart, liver, and brains.
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Animal Model:Wistar rats [1]
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Dosage:20mg/kg for 9 days
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Administration:Oral gavage (p.o.)
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Result:Decreased the ELT and increased total platform crossing as compared to the diseased model group
. Increased the neuronal density and neuronal arrangement.
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Animal Model:Wistar rats[1]
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Dosage:10 and 20 mg/kg for 4 days
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Administration:i.g.
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Result:The concentrations of AK-2 in brain homogenates were observed to 0.633 and 0.977 μg/mL.
Chemical Information
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CAS No. 229476-71-5
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Molecular Weight 364.44
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Formula C21H24N4O2
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SMILES
COC1=C(OC)C=C2C(N(CC3)CCN3CC4=CC=CC=C4)=NC=NC2=C1
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
hAChE/hBACE-1-IN-4 Related Classifications
HY-161512 Related Classifications
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