2. Neuronal Signaling NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Cholinesterase (ChE) Reactive Oxygen Species (ROS)
  4. AChE/BChE-IN-27

AChE/BChE-IN-27 is a blood-brain barrier–permeable mixed inhibitor (Pe = 4.12) of AChE and BChE, with IC50 values of 3.72 μM and 9.65 μM, respectively. AChE/BChE-IN-27 has potent antioxidant activity with an IC50 value of 6.32 μM in the DPPH (HY-112053) assay and also exhibits potent in vitro antioxidant activity. AChE/BChE-IN-27 exhibits metal chelating properties. AChE/BChE-IN-27 has neuroprotective potential against oxidative stress. AChE/BChE-IN-27 significantly reduces intracellular reactive oxygen species (ROS). In in vivo experiments, AChE/BChE-IN-27 effectively restored AChE and BChE levels, improved cognition, and can be used for Alzheimer's disease (AD).

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AChE/BChE-IN-27 Chemical Structure

AChE/BChE-IN-27 Chemical Structure

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AChE/BChE-IN-27 Related Antibodies

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Description

AChE/BChE-IN-27 is a blood-brain barrier–permeable mixed inhibitor (Pe = 4.12) of AChE and BChE, with IC50 values of 3.72 μM and 9.65 μM, respectively. AChE/BChE-IN-27 has potent antioxidant activity with an IC50 value of 6.32 μM in the DPPH (HY-112053) assay and also exhibits potent in vitro antioxidant activity. AChE/BChE-IN-27 exhibits metal chelating properties. AChE/BChE-IN-27 has neuroprotective potential against oxidative stress. AChE/BChE-IN-27 significantly reduces intracellular reactive oxygen species (ROS). In in vivo experiments, AChE/BChE-IN-27 effectively restored AChE and BChE levels, improved cognition, and can be used for Alzheimer's disease (AD)[1].

IC50 & Target

hAChE

3.72 μM (IC50)

eqBCHE

9.65 μM (IC50)

In Vitro

AChE/BChE-IN-27 (Compound 12d) (10 nM-100 μM 12 days) shows the high inhibitory effects with IC50 values of 3.72 μM (AChE) and 9.65 μM (BChE)[1].

AChE/BChE-IN-27 (1-30 μM, 37 °C, 30 min) exhibits mixed inhibitory effects on hAChE and eqBChE in enzyme kinetic assays[1].

AChE/BChE-IN-27 (5-50 μM, 25 °C, 6 h) shows a PI displacement of 23.58 % in peripheral anionic site (PAS) inhibition studies against AChE[1].

AChE/BChE-IN-27 (1.25-20 μM, 37 °C, 30 min) shows the most potent antioxidant activity in the DPPH (HY-112053) assay with an IC50 value of 6.32 μM[1].

AChE/BChE-IN-27 (500 μM, 37 °C, 18 h) exhibits a Pe value greater than 2.0, suggesting moderate BBB permeability (CNS ±)[1].

AChE/BChE-IN-27 (18 μM, 5 min) could serve as a potential therapeutic agent for mitigating metal ion dysregulation[1].

AChE/BChE-IN-27 (5 μM, 37 °C, 72 h) inhibits Aβ1-42 aggregation, results in the inhibition of Aβ1–42 fibril formation, demonstrating its potential as an aggregation modulator[1].

AChE/BChE-IN-27 (5-80 μM, 24 h) shows no cytotoxicity in SH-SY5Y cells[1].

AChE/BChE-IN-27 (5-80 μM, 24 h) can effectively protect SH-SY5Y cells from H2O2-induced neurotoxicity[1].

AChE/BChE-IN-27 (1-80 μM, 24 h) reduces ROS levels and protects cells in SH-SY5Y cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AChE/BChE-IN-27 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 80, 60, 50, 40, 20, 10, and 5 μM
Incubation Time: 24 h
Result: Showed no cytotoxicity in SH-SY5Y cells.
In Vivo

AChE/BChE-IN-27 (Compound 12d) (500 mg/kg, p.o., once) is not toxic in male Swiss albino mice[1].

AChE/BChE-IN-27 (1-10 mg/kg, i.p., once a day, 7 days) exhibits significant anti-ChE activity and improves cognitive function in the scopolamine-induced amnesia model, has dual pharmacological activity as a cholinesterase inhibitor and a potent antioxidant[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Scopolamine-induced Alzheimer's mice, albino mice of both sexes (male and female) weighing 25 and 30 g[1]
Dosage: 1 mg/kg , 5 mg/kg, 10 mg/kg
Administration: i.p., once a day, 7 days
Result: Exhibited significant anti-ChE activity and improves cognitive function, improved spatial working memory.
Attenuates the increased AChE and BChE activities after scopolamine administration, restored the decreased SOD level caused by scopolamine-induced oxidative stress.
Molecular Weight

379.41

Formula

C21H21N3O4
SMILES

O=C(CNC(/C=C/C1=CC(O)=C(C=C1)O)=O)NCCC2=CNC3=CC=CC=C23
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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AChE/BChE-IN-27 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:

AChE/BChE-IN-27Cholinesterase (ChE)Reactive Oxygen Species (ROS)InhibitorSH-SY5Y cellsScopolamine-induced Alzheimer's miceAlzheimer's diseaseinhibitorinhibit

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