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).
For research use only. We do not sell to patients.
- Formula: C21H21N3O4
- Molecular Weight:379.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
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. Further protocols information, click here.
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Cell Line:SH-SY5Y cells
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Concentration:80, 60, 50, 40, 20, 10, and 5 μM
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Incubation Time:24 h
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Result:Showed no cytotoxicity in SH-SY5Y cells.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-t | Brain distribution |
|---|---|---|---|---|---|---|---|
| Rat | 5 mg/kg | i.p. | 0.49 μg/mL | 8 h | 4.77 h | 7.36 μg/mL·h | 0.37 μg/mL |
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.
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Animal Model:Scopolamine-induced Alzheimer's mice, albino mice of both sexes (male and female) weighing 25 and 30 g[1]
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Dosage:1 mg/kg , 5 mg/kg, 10 mg/kg
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Administration:i.p., once a day, 7 days
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Result:Exhibited significant anti-ChE activity and improves cognitive function, improved spatial working memory.
Attenuated the increased AChE and BChE activities after scopolamine administration, restored the decreased SOD level caused by scopolamine-induced oxidative stress.
Chemical Information
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Molecular Weight 379.41
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Formula C21H21N3O4
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SMILES
O=C(CNC(/C=C/C1=CC(O)=C(C=C1)O)=O)NCCC2=CNC3=CC=CC=C23
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AChE/BChE-IN-27 Related Classifications
HY-174399 Related Classifications
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