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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C24H28N4O3
- 分子量:420.50
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保管条件:
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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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
COX-2 0.11 μM (IC50) |
hBCHE 1.48 nM (IC50) |
eqBCHE 74.4 pM (IC50) |
体外実験
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.
体内実験
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.
化学情報
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分子量 420.50
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
BChE-IN-46 関連分類
HY-179363 関連分類
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