hAChE/hBACE-1-IN-2

Cat. No.: HY-149288: FAQs
Data Sheet Handling Instructions

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hAChE/hBACE-1-IN-2 is a potent, orally active, blood-brain barrier transboundary triple inhibitor of hAChE, hBChE, and HACE-1 with IC₅₀s of 0.113 μM, 1.48 μM and 0.38 μM, respectively. hAChE/hBACE-1-IN-2 has antioxidant activity. hAChE/hBACE-1-IN-2 also inhibits Aβ1_1-42 aggregation. hAChE/hBACE-1-IN-2 can be used to study Alzheimer's disease.

For research use only. We do not sell to patients.

hAChE/hBACE-1-IN-2 Chemical Structure

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

hAChE

0.113 μM (IC₅₀)

hBACE-1

0.38 μM (IC₅₀)

hBCHE

1.48 μM (IC₅₀)

In Vitro

hAChE/hBACE-1-IN-2 (compound 5f) (10-80 μM; 72 h) is considered similar to Donepezil (HY-14566) in terms of safety in SH-SY5Y neuroblastoma cell lines^[1].
hAChE/hBACE-1-IN-2 (compound 5f) (20 μM; 48 h, 72 h) has the potential of anti-Aβ_1-42 aggregation potential in SH-SY5Y neuroblastoma cell lines^[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 cell lines (The SH-SY5Y cells were sequentially treated with RA and BDNF for 6 days)
Concentration:	10, 20, 40, and 80 μM
Incubation Time:	48-72 h
Result:	Indicated a similar reduction in the differentiated neuroblastoma cell population at a maximum 80 μM concentration.

Cell Viability Assay^[1]

Cell Line:	Aβ_1-42 treated SH-SY5Y cells (incubated with Aβ_1-42 (10μM) for 24 h)
Concentration:	20 μM
Incubation Time:	48-72 h
Result:	The cells incubated the cell viability to 65% and 75% after 48 h and 72 h.

In Vivo

hAChE/hBACE-1-IN-2 (2.5-10 mg/kg/day, p.o., 14 days) improves learning and memory and reduce RTL and time spent in open arms in the Scopolamine (HY-N0296)-induced cognitive deficit mouse model^[1].
hAChE/hBACE-1-IN-2 (500 mg/kg, p.o., 14 days) is well tolerated and has no apparent toxicity in Swiss albino mice, including brain, liver, kidneys, and heart abnormalities^[1].
hAChE/hBACE-1-IN-2 (10 mg/kg, p.o., 14 days) crosses the blood-brain barrier, reduces AchE levels or substrate hydrolysis in hippocampal and cortical brain homogenates, delays oxidative stress and reduces the potential for pro-inflammatory cytokine levels in a mouse model induced by Scopolamine (HY-N0296)^[1].
hAChE/hBACE-1-IN-2 (10 mg/kg, p.o., 14 days) inhibits BACE-1, Aβ, APP/Aβ, and tau protein, protect 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:	Swiss albino mice^[1]
Dosage:	500 mg/kg
Administration:	Oral administration (p.o.), 14 days
Result:	Showed no signs or symptoms of toxicity over the 14 days

Animal Model:	Scopolamine-induced cognitive deficit mouse model^[1]
Dosage:	2.5 mg, 5 mg, and 10 mg/kg
Administration:	Oral administration (p.o.), 14 days
Result:	Elevated plus maze test showed significant reductions in transfer latency and time spent in open arms, similar to the effects observed with Scopolamine (HY-N0296)-induced dementia reversal.

Molecular Weight

408.52

Formula

C₂₂H₂₄N₄O₂S

SMILES

O=C(CSC1=NN=C(C2=CC=CC=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-2 Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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-2Cholinesterase (ChE)Beta-secretaseAmyloid-βBACEβ-Secretase β-amyloid peptideAβAbetaSH-SY5Yblood-brain barrierMTDLscopolamine-induced amnesia modelAlzheimer’s diseaseInhibitorinhibitorinhibit

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