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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- Formel: C21H21N3O4
- Molecular Weight:379.41
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
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hAChE 3.72 μM (IC50) |
eqBCHE 9.65 μM (IC50) |
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.
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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.
| 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 |
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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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AChE/BChE-IN-27 Related Classifications
HY-174399 Related Classifications
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