hAChE-IN-8
hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research.
For research use only. We do not sell to patients.
- Formula: C25H22N4O4
- Molecular Weight:442.47
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
hBCHE 0.542 μM (IC50) |
DYRK1A >10 μM (IC50) |
hAChE 0.486 μM (IC50) |
In Vitro
hAChE-IN- 8 (10-80 μM; 72 h) is not toxic to SH-SY5Y neuronal cells at high concentrations[1].
hAChE-IN- 8 (40 μM; 72 h) protects SH-SY5Y cells from Aβ1-42-induced oxidative stress with significantly increase in survival and normalization of cell morphology[1].
hAChE-IN- 8 (5-20 μM; 48 h) shows significant anti-Aβ aggregation activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
hAChE-IN- 8 (2.5-10 mg/kg; p.o.; single dose) improves scopolamine (HY-N0296) -induced memory loss in a dose-dependent manner. Shows antioxidant potential in scopolamine-induced oxidative stress and restores ACh and AChE levels[1].
hAChE-IN- 8 (10 mg/kg; p.o.; once daily for 9 days) Aβ1-42 shows significant cognitive improvement in the Aβ1-42 induced AD model. Significantly reduces AD-related protein levels[1].
hAChE-IN- 8 (10-200 μM) is added to the culture medium of Drosophila and shows no significant toxicity to Drosophila at lower concentrations, but exhibits some toxicity at higher concentrations[1].
hAChE-IN- 8 (10-20 μM) effectively restores Aβ42-induced ocular phenotypic changes in the Drosophila AD model, exhibiting significant neuroprotective effects[1].
hAChE-IN- 8 (5-50 μM) exhibits a high viability of larval cells at lower concentrations, but at higher concentrations the cell viability decreases significantly and exhibits some cytotoxicity[1].
Pharmacokinetic Analysis in Wistar rat[1]
| Route | Dose (mg/kg) | Tmax (h) | Cmax (ng/mL) | t1/2 (h) | MRT (h) | AUC0-8 (ng/mL.h) | AUCtotal (ng/mL.h) |
| p.o. | 10 | 9 ± 1.041 | 355 ± 6.033 | 41 ± 1.017 | 32 ± 1.713 | 1136.18 ± 4.017 | 1736.18 ± 7.101 |
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:500,1000 mg/kg
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Administration:p.o.; single dose
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Result:At the maximum dose of 1000 mg/kg, the histology of organs (kidney, liver, brain and heart) was normal in rats after 14 days.
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Animal Model:Scopolamine-induced memory loss in Wistar rats[1]
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Dosage:2.5 mg/kg, 5 mg/kg, 10 mg/kg
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Administration:p.o.; single dose
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Result:The effect of improvement in the 10 mg/kg dose group was similar to donepezil (HY-14566) group. Decreased AChE activity, increased ACh levels, decreased MDA levels, and increased SOD, CAT, and GSH levels.
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Animal Model:Aβ1-42 induced AD mode[1]
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Dosage:10 mg/kg
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Administration:p.o.; once daily for 9 days
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Result:Significantly reduced escape latency (ELT) and increased number of plateau crossings, similar to the donepezil (HY-14566) group. Significantly reduced BACE-1, α-synuclein, APP and Tau protein levels. Significantly reduced BACE-1 and Aβ levels in the DG, CA1 and CA3 regions.
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Animal Model:AD Drosophila model [1]
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Dosage:10 μM, 20 μM
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Administration:/
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Result:At a concentration of 10 μM, the recovery of the eye phenotype in Drosophila was 21%. At 20 μM, the recovery rate increased to 57%.
Chemical Information
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Molecular Weight 442.47
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Formula C25H22N4O4
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SMILES
COC1=CC(NC(CN2N=C(C(C3=CC=CC=C3)=NC2=O)C4=CC=CC=C4)=O)=CC(OC)=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.
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.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
hAChE-IN-8 Related Classifications
HY-163514 Related Classifications
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