2. Neuronal Signaling
  3. Cholinesterase (ChE) Beta-secretase Amyloid-β
  4. hAChE/hBACE-1-IN-2

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 Aβ11-42 aggregation. hAChE/hBACE-1-IN-2 can be used to study Alzheimer's disease.

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hAChE/hBACE-1-IN-2 Chemical Structure

hAChE/hBACE-1-IN-2 Chemical Structure

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hAChE/hBACE-1-IN-2 Related Antibodies

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AChE BChE

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Description

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 Aβ11-42 aggregation. hAChE/hBACE-1-IN-2 can be used to study Alzheimer's disease[1].

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-Aβ1-42 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.

hAChE/hBACE-1-IN-2 Related Antibodies

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: Aβ1-42 treated SH-SY5Y cells (incubated with Aβ1-42 (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
References
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hAChE/hBACE-1-IN-2 Related Classifications

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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)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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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/hBACE-1-IN-2Cholinesterase (ChE)Beta-secretaseAmyloid-βBACEβ-Secretase β-amyloid peptideAβAbetaSH-SY5Yblood-brain barrierMTDLscopolamine-induced amnesia modelAlzheimer’s diseaseInhibitorinhibitorinhibit

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