BChE-IN-44
BChE-IN-44 is a potent, brain-penetrant, highly selective BChE inhibitor [equine BChE IC50 = 18.00 pM, human BChE IC50 = 1.50 nM]. BChE-IN-44 shows neuroprotective effects against the Aβ1-42-induced injury model and inhibitory effects on Aβ1-42 self-aggregation. BChE-IN-44 reduces the levels of inflammatory factors (NO, IL-6, and TNF-α) in Lipopolysaccharides (HY-D1056)-induced BV2 cells. BChE-IN-44 can significantly ameliorate Scopolamine (HY-N0296)-induced cognition impairment. BChE-IN-44 exhibits capacity in the regulation of BChE and acetylcholine levels in the mouse hippocampus. BChE-IN-44 can be used for the study of Alzheimer’s disease (AD).
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: C22H23N3O4
- 分子量:393.44
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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
- 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
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IL-6 |
RatBuChE |
体外実験
BChE-IN-44 (Compound N14) (50 μM, 24 h) lead to about 15 % cell toxicity in PC12 and SH-SY5Y, suggesting that BChE-IN-44 possesses a high safety profile in vitro[1].
BChE-IN-44 shows a Kc of 0.017 μM, indicating that BChE-IN-44 possesses a higher affinity for BChE[1].
BChE-IN-44 (5-20 μM, 24 h) significantly reduces the levels of inflammatory factors (NO, IL-6, and TNF-α) in Lipopolysaccharides (LPS)-induced BV2 cells[1].
BChE-IN-44 (20 μM, 24 h) demonstrates significant neuroprotective efficacy against Aβ1–42-induced injury in PC12 cells[1].
BChE-IN-44 (20 μM, 48 h) effectively inhibits Aβ1-42 aggregation, confirming the good inhibitory effects of the carrier scaffold on Aβ1–42 aggregation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC12 cells, SH-SY5Y cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Led to about 15 % cell toxicity in PC12 and SH-SY5Y.
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Cell Line:BV2 cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:24 h
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Result:Significantly reduced the levels of inflammatory factors (NO, IL-6, and TNF-α) in LPS-induced BV2 cells.
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Cell Line:PC12 cells
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Concentration:20 nM
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Incubation Time:24 h
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Result:Showed significant neuroprotective efficacy against Aβ1-42-induced injury in PC12 cells.
Parmacokinetics
| Species | Dose | Route | AUC0-t | MRT0-t | T1/2 | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|
| Rat | 5 mg/kg | i.v. | 9.94 μg·h/mL | 0.75 h | 3.1 h | 27.87 μg/mL | 0.033 h | / |
| Rat | 50 mg/kg | i.p. | 16.36 μg·h/mL | 2.57 h | 4.43 h | 12.93 μg/mL | 0.25 h | 16.46 % |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Thirty-six six-week-old male Kunming mice (weighing 25-30 g) were intraperitoneally injected with scopolamine (3 mg/kg) to mimic AD-like cognitive deficits[1].
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Dosage:5 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:I.p., once daily for 14 days, 30 mins after Scopolamine
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Result:Increased the spontaneous alternation rate to 72.6%, indicating improved working memory.
Increased central region dwell time and travel distance, and reduced anxiety-like behaviors.
Shortened escape latency, reduced travel distance, and increased platform crossings, showing improved spatial learning memory.
Behavioral trajectory plots showed more organized.
Increases ACh levels and decreases AChE and BChE activities.
Reduces IL-6 and TNF-α levels and inhibits neuroinflammation.
化学情報
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分子量 393.44
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分子式 C22H23N3O4
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SMILES
CC1=CC(O)=C(C=C1)C(NCCC2=CNC3=CC=C(C=C23)OC(N4CCC4)=O)=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.
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-44 関連分類
HY-178356 関連分類
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