BChE-IN-46
BChE-IN-46 is a selective and brain-penetrant BChE inhibitor (eqBChE IC50 = 7.44 × 10−5 μM, SI > 270,000; hBChE, IC50 = 1.48 × 10−3 μM). BChE-IN-46 has COX-2 inhibitory activity (IC50 = 0.11 μM). BChE-IN-46 exhibits neuroprotective effects, enhances acetylcholine levels, and alleviates cognitive deficits, anxiety, and learning/memory impairments. BChE-IN-46 can be used for the development of anti-Alzheimer's disease drugs.
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- Fòrmula: C24H28N4O3
- Peso molecular:420.50
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Actividad biológica
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COX-2 0.11 μM (IC50) |
hBCHE 1.48 nM (IC50) |
eqBCHE 74.4 pM (IC50) |
BChE-IN-46 (Compound 17) (100 μM, 24 h) possesses the promising in vitro cell safety in BV2, PC12 and HT22 cell[1].
BChE-IN-46 (5-20 μM, 24 h) has anti-inflammatory activity in Lipopolysaccharides (LPS) (HY-D1056)-induced BV2 cells[1].
BChE-IN-46 (10-40 μM, 24 h) has neuroprotective effects against Aβ in β-Amyloid (1-42) (Aβ1-42) (HY-P1363)-induced injury in PC12 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BV2, PC12 and HT22 cell
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Concentration:100 μM
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Incubation Time:24 h
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Result:Exhibited weak or no toxicity on BV2, PC12 and HT22 cell.
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Cell Line:LPS (1 μg/mL)-induced BV2 cells
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Concentration:5, 10, and 20 μM
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Incubation Time:24 h
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Result:Reduced LPS-induced NO, IL-6, and TNF-α production in a concentration-dependent manner.
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Cell Line:Aβ1-42-induced PC12 cell
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Concentration:10, 20, and 40 μM
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Incubation Time:24 h
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Result:Exhibited a dose-dependent protection against Aβ1-42-induced toxicity in PC12 cells and the protective efficacy.
BChE-IN-46 (250 mg/kg, i.p., once) inherits favorable in vivo safety in Kunming mice[1].
BChE-IN-46 (100 mg/kg, i.p., once) has effective BBB penetration and CSF retention in male SD rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Scopolamine (3 mg/kg, i.p.) -induced male Kunming mice (25 g-30 g, 6 weeks)[1].
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Dosage:3, 12.5, 25 mg/kg
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Administration:i.p., once daily, 16 days
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Result:Increased both movement distance and residence time in the central region.
Produces no cholinergic adverse effects or motor deficits in mice.
Reduced path length.
Ameliorated scopolamine-induced cholinergic dysfunction primarily through BChE inhibition-mediated ACh restoration.
Attenuated increases in hippocampal TNF-α and IL-6.
Reversed the scopolamine-induced reduction in Nissl positive neurons and ameliorated neuronal damage.
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Animal Model:Kunming mice (30 g-35 g, 6 weeks)[1].
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Dosage:250 mg/kg
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Administration:i.p., once, dissolved in a mixed solvent composed of DMSO (HY-Y0320C), HS-15 (HY-Y1893), castor oil (HY-107799) and normal saline (HY-W460471) (8/5/5/82, V/V/V/V).
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Result:Had no mortality or treatment-related abnormalities.
Did not significantly alter the mean body weight.
Resulted in normal tissue architecture in major organs, with no treatment-related lesions observed.
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Animal Model:male SD rats (220 g-250 g, 8 weeks)[1].
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Dosage:100 mg/kg
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Administration:i.p., once
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Result:Maintained sustained concentrations in cerebrospinal fluid (CSF) between 20 min and 2 h.
Chemical Information
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Peso molecular 420.50
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Fòrmula C24H28N4O3
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SMILES
CC(C=C1)=CC(OC(N2CCC2)=O)=C1C(NCCC3=CNC4=CC(N(C)C)=CC=C43)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BChE-IN-46 Related Classifications
HY-179363 Related Classifications
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