2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Cholinesterase (ChE) DYRK
  4. 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.

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hAChE-IN-8 Chemical Structure

hAChE-IN-8 Chemical Structure

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hAChE-IN-8 Related Antibodies

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Description

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[1].

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.

hAChE-IN-8 Related Antibodies
In Vivo

hAChE-IN- 8 (500,1000 mg/kg; p.o.; single dose) at the high dose shows no toxicity or abnormal response in all Wistar rats during the 14-day observation period[1].
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.

Animal Model: Wistar rats[1]
Dosage: 500,1000 mg/kg
Administration: p.o.; single dose
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.
Animal Model: Scopolamine-induced memory loss in Wistar rats[1]
Dosage: 2.5 mg/kg, 5 mg/kg, 10 mg/kg
Administration: p.o.; single dose
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.
Animal Model: Aβ1-42 induced AD mode[1]
Dosage: 10 mg/kg
Administration: p.o.; once daily for 9 days
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.
Animal Model: AD Drosophila model [1]
Dosage: 10 μM, 20 μM
Administration: /
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%.
Molecular Weight

442.47

Formula

C25H22N4O4
Unlabeled CAS

SMILES

COC1=CC(NC(CN2N=C(C(C3=CC=CC=C3)=NC2=O)C4=CC=CC=C4)=O)=CC(OC)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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hAChE-IN-8 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

hAChE-IN-8Cholinesterase (ChE)DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseMTDLAlzheimer's diseaseAChE inhibitorAnti-Aβ aggregationNeuroprotective effectsDrosophila modelWistar ratsInhibitorinhibitorinhibit

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