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.
For research use only. We do not sell to patients.
- Formula: C24H28N4O3
- Molecular Weight:420.50
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
COX-2 0.11 μM (IC50) |
hBCHE 1.48 nM (IC50) |
eqBCHE 74.4 pM (IC50) |
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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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Molecular Weight 420.50
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Formula 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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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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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)
BChE-IN-46 Related Classifications
HY-179363 Related Classifications
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