hAChE-IN-8
hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research.
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: C25H22N4O4
- 分子量:442.47
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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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hBCHE 0.542 μM (IC50) |
DYRK1A >10 μM (IC50) |
hAChE 0.486 μM (IC50) |
hAChE-IN- 8 (10-80 μM; 72 h) is not toxic to SH-SY5Y neuronal cells at high concentrations[1].
hAChE-IN- 8 (40 μM; 72 h) protects SH-SY5Y cells from Aβ1-42-induced oxidative stress with significantly increase in survival and normalization of cell morphology[1].
hAChE-IN- 8 (5-20 μM; 48 h) shows significant anti-Aβ aggregation activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
hAChE-IN- 8 (2.5-10 mg/kg; p.o.; single dose) improves scopolamine (HY-N0296) -induced memory loss in a dose-dependent manner. Shows antioxidant potential in scopolamine-induced oxidative stress and restores ACh and AChE levels[1].
hAChE-IN- 8 (10 mg/kg; p.o.; once daily for 9 days) Aβ1-42 shows significant cognitive improvement in the Aβ1-42 induced AD model. Significantly reduces AD-related protein levels[1].
hAChE-IN- 8 (10-200 μM) is added to the culture medium of Drosophila and shows no significant toxicity to Drosophila at lower concentrations, but exhibits some toxicity at higher concentrations[1].
hAChE-IN- 8 (10-20 μM) effectively restores Aβ42-induced ocular phenotypic changes in the Drosophila AD model, exhibiting significant neuroprotective effects[1].
hAChE-IN- 8 (5-50 μM) exhibits a high viability of larval cells at lower concentrations, but at higher concentrations the cell viability decreases significantly and exhibits some cytotoxicity[1].
Pharmacokinetic Analysis in Wistar rat[1]
| Route | Dose (mg/kg) | Tmax (h) | Cmax (ng/mL) | t1/2 (h) | MRT (h) | AUC0-8 (ng/mL.h) | AUCtotal (ng/mL.h) |
| p.o. | 10 | 9 ± 1.041 | 355 ± 6.033 | 41 ± 1.017 | 32 ± 1.713 | 1136.18 ± 4.017 | 1736.18 ± 7.101 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats[1]
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Dosage:500,1000 mg/kg
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Administration:p.o.; single dose
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Result:At the maximum dose of 1000 mg/kg, the histology of organs (kidney, liver, brain and heart) was normal in rats after 14 days.
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Animal Model:Scopolamine-induced memory loss in Wistar rats[1]
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Dosage:2.5 mg/kg, 5 mg/kg, 10 mg/kg
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Administration:p.o.; single dose
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Result:The effect of improvement in the 10 mg/kg dose group was similar to donepezil (HY-14566) group. Decreased AChE activity, increased ACh levels, decreased MDA levels, and increased SOD, CAT, and GSH levels.
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Animal Model:Aβ1-42 induced AD mode[1]
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Dosage:10 mg/kg
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Administration:p.o.; once daily for 9 days
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Result:Significantly reduced escape latency (ELT) and increased number of plateau crossings, similar to the donepezil (HY-14566) group. Significantly reduced BACE-1, α-synuclein, APP and Tau protein levels. Significantly reduced BACE-1 and Aβ levels in the DG, CA1 and CA3 regions.
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Animal Model:AD Drosophila model [1]
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Dosage:10 μM, 20 μM
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Administration:/
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Result:At a concentration of 10 μM, the recovery of the eye phenotype in Drosophila was 21%. At 20 μM, the recovery rate increased to 57%.
化学情報
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分子量 442.47
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分子式 C25H22N4O4
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SMILES
COC1=CC(NC(CN2N=C(C(C3=CC=CC=C3)=NC2=O)C4=CC=CC=C4)=O)=CC(OC)=C1
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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)
hAChE-IN-8 関連分類
HY-163514 関連分類
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