AChE-IN-94
AChE-IN-94 is an orally active and blood-brain barrier penetrable AChE inhibitor with an IC50 of 0.40 μM and Ki of 0.28 μM. AChE-IN-94 prevents self-induced and AChE-mediated Aβ1-42 aggregation. AChE-IN-94 alleviates cognitive/memory deficits in Scopolamine (HY-N0296)-induced amnesic model. AChE-IN-94 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: C20H18ClFN4O2S
- 分子量:432.90
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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
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AChE 0.4 μM (IC50) |
AChE 0.28 μM (Ki) |
AChE-IN-94 (Compound LB05) exhibits potent inhibitory activity against AChE with an IC50 of 0.40 μM and an inhibition constant (Ki) of 0.28 μM[1].
AChE-IN-94 (10-50 μM) displaces propidium iodide (PI) from the peripheral anionic site (PAS) of AChE in a dose-dependent manner[1].
AChE-IN-94 (5-20 μM, 48 h incubation, in vitro) inhibits Aβ₁₋₄₂ aggregation in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax | AUC | T1/2 | CL/F | Vd/F | MRT |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.g. | 6.76 μg/mL | 2 h | 39.34 μg·h/mL | 6.11 h | 190 mL/h/kg | 1540 mL/kg | 9.65 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Scopolamine-induced amnesia rat model: Male Wistar rats (160-180 g) were injected with scopolamine (3 mg/kg, i.p.) on the 7th day[1]
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Dosage:5, 10, 20 mg/kg
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Administration:p.o., once daily for 7 days
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Result:Ameliorated cognitive deficits in a dose-dependent manner.
Restored the percentage of spontaneous alternation (reflecting spatial working memory) and the total number of arm entries (reflecting exploratory activity).
Improved cholinergic function and reduced oxidative stress in the hippocampus.
Decreased AChE activity, reduced malondialdehyde (MDA) levels, and elevated catalase (CAT) activity.
化学情報
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分子量 432.90
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分子式 C20H18ClFN4O2S
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SMILES
O=C(NC1=NC2=CC=C(Cl)C=C2S1)CN3CCN(C(C4=CC=C(F)C=C4)=O)CC3
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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)
AChE-IN-94 関連分類
HY-175758 関連分類
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