hAChE/hBACE-1-IN-1
hAChE/hBACE-1-IN-1 (compounds 5d) is an orally active inhibitor of hAChE with blood-brain permeability. hAChE/hBACE-1-IN-1 inhibits hAChE and hBACE-1 with IC50 values of 0.076 and 0.23 μM, respectively. hAChE/hBACE-1-IN-1 inhibits Aβ1-42 aggregation and improves mouse learning and memory ability. hAChE/hBACE-1-IN-1 can be used to research in Alzheimer's disease.
For research use only. We do not sell to patients.
- Formula: C23H23N5O2S
- Molecular Weight:433.53
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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hAChE 0.076 μM (IC50) |
hBACE-1 0.23 μM (IC50) |
hBCHE 1.204 μM (IC50) |
hAChE/hBACE-1-IN-1 (10-80 μM, 48 h) has safety at maximum concentration in SH-SY5Y cell[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 μM, 20 μM, 40 μM, 80 μM
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Incubation Time:48 h, 72 h
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Result:Indicated the similar in safety to donepezil (HY-14566) at a maximum 80 μM concentration.
Restored the cell that Aβ1-42 treated viability to 70% after 48 h, to 77% after 72 h cell.
hAChE and hBACE-1 inhibitors (500 mg/kg, p.o., 30 days) is well tolerated and has no apparent toxicity to mice, including brain, liver, kidneys, and heart abnormalities[1].
hAChE/hBACE-1-IN-1 (10 mg/kg, p.o., 14 days) is capable of crossing the blood-brain barrier, decreases AChE levels or substrate hydrolysis in hippocampal and cortex brain homogenates, has the potential to retard the oxidative stress and reduces levels of proinflammatory cytokines induced by scopolamine [1].
hAChE/hBACE-1-IN-1 (10 mg/kg, p.o., 14 days) inhibits BACE-1, Aβ, APP/Aβ, and tau protein, protects brain tissue in different brain regions in the Aβ-induced model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:scopolamine-induced amnesia models in Swiss albino mice[1].
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Dosage:2.5, 5, 10 mg/kg/day
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Administration:oral administration (p.o.) 14 days
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Result:Improved learning and memory and reduce RTL and time spent in open arms.
Crossed the blood-brain barrier, and reduced AChE levels or substrate hydrolysis in hippocampal and cortex brain homogenates.
Reduced MDA, ROS levels, nitrite concentration, and increased GSH levels in a dose-dependent manner.
Reduced levels of proinflammatory cytokines.
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Animal Model:Aβ-induced models in Swiss albino mice[1].
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Dosage:10 mg/kg/day
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Administration:oral administration (p.o.) 14 days
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Result:Inhibited BACE-1, Aβ, APP/Aβ, and tau protein and protected brain tissue in different brain regions.
Chemical Information
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Molecular Weight 433.53
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Formula C23H23N5O2S
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SMILES
O=C(CSC1=NN=C(C2=CC=CC(C#N)=C2)O1)NC3CCN(CC3)CC4=CC=CC=C4
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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-1 Related Classifications
HY-149287 Related Classifications
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