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

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 Aβ1-42 aggregation and improves mouse learning and memory ability. hAChE/hBACE-1-IN-1 can be used to research in Alzheimer's disease.

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hAChE/hBACE-1-IN-1 Chemical Structure

hAChE/hBACE-1-IN-1 Chemical Structure

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hAChE/hBACE-1-IN-1 Related Antibodies

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Description

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 Aβ1-42 aggregation and improves mouse learning and memory ability. hAChE/hBACE-1-IN-1 can be used to research in Alzheimer's disease[1].

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.

hAChE/hBACE-1-IN-1 Related Antibodies

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 Aβ1-42 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
References
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hAChE/hBACE-1-IN-1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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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