hAChE/hBACE-1-IN-1

Cat. No.: HY-149287: FAQs
Data Sheet Handling Instructions

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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 Aβ_1-42 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.

hAChE/hBACE-1-IN-1 Chemical Structure

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AChE BChE

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Purity & Documentation
References
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Description

IC₅₀ & Target

hAChE

0.076 μM (IC₅₀)

hBACE-1

0.23 μM (IC₅₀)

hBCHE

1.204 μM (IC₅₀)

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:	SH-SY5Y
Concentration:	10 μM, 20 μM, 40 μM, 80 μM
Incubation Time:	48 h, 72 h
Result:	Indicated the similar in safety to donepezil (HY-14566) at a maximum 80 μM concentration. Restored the cell that Aβ_1-42 treated viability to 70% after 48 h, to 77% after 72 h cell.

In Vivo

hAChE/hBACE-1-IN-1 (2.5-10 mg/kg/day, p.o., 14 days) improves learning and memory and reduces RTL and time spent in open arms in the scopolamine-induced cognitive deficit mouse model^[1].
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.

Animal Model:	scopolamine-induced amnesia models in Swiss albino mice^[1].
Dosage:	2.5, 5, 10 mg/kg/day
Administration:	oral administration (p.o.) 14 days
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.

Animal Model:	Aβ-induced models in Swiss albino mice^[1].
Dosage:	10 mg/kg/day
Administration:	oral administration (p.o.) 14 days
Result:	Inhibited BACE-1, Aβ, APP/Aβ, and tau protein and protected brain tissue in different brain regions.

Molecular Weight

433.53

Formula

C₂₃H₂₃N₅O₂S

SMILES

O=C(CSC1=NN=C(C2=CC=CC(C#N)=C2)O1)NC3CCN(CC3)CC4=CC=CC=C4

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

Handling Instructions (2659 KB)

References

[1]. Waiker DK, et al. Design, Synthesis, and Biological Evaluation of Piperazine and N-Benzylpiperidine Hybrids of 5-Phenyl-1,3,4-oxadiazol-2-thiol as Potential Multitargeted Ligands for Alzheimer's Disease Therapy. ACS Chem Neurosci. 2023 Jun 7;14(11):2217-2242. [Content Brief]

hAChE/hBACE-1-IN-1 Related Classifications

Neurological Disease

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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/hBACE-1-IN-1Cholinesterase (ChE)SH-SY5Yblood-brain barrierMTDLscopolamine-induced amnesia modelAlzheimer’s diseaseInhibitorinhibitorinhibit

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