AMG-8718
AMG-8718 is a potent, selective and orally active BACE1 inhibitor with IC50 values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ40 levels in the CSF and brain.
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。
- CAS 番号: 1215868-94-2
- 分子式: C25H19FN4O3
- 分子量:442.44
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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
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BACE1 0.0007 μM (IC50) |
BACE2 0.005 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
4.4 nM
Compound: 42, AMG-8718
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Inhibition of BACE1 in HEK293 cells assessed as Abeta40 level after overnight incubation by sandwich ELISA
Inhibition of BACE1 in HEK293 cells assessed as Abeta40 level after overnight incubation by sandwich ELISA
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[PMID: 25363711] |
AMG-8718 (compound 42) shows good stability in human and rat liver microsomes, hERG binding activity with an Ki value of >10 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AMG-8718 (i.v. for 2 mg/kg or p.o. for 5 mg/kg) shows good bioavailability of 70%, 96%,101% for rats, beagle dog, monkey, respectively[1].
AMG-8718 (30 mg/kg for; p.o.) dose-dependent decreases in both CSF and brain Aβ levels at 4 h time points with 50% Aβ reduction (EC50) values of 18 and 67 nM for CSF and brain respectively in rats[1].
AMG-8718 (2.5, 8, 16 mg/kg; i.v.; a series of three 30 min infusions) shows high unbound plasma concentrations with 0.298, 1.70, 3.62 µM at the end of each infusion in chloralose-anesthetized dogs[1].
Pharmacokinetic Parameters ofAMG-8718 in rats, beagle dog, cynomolgus monkey[1].
| species | Cl (L/h/kg) | Vdss(L/kg) | t1/2(h) | Cmax (µM) | tmax(h) | % F | plasma protein binding (Fu) | |
| i.v. | p.o. | |||||||
| rat | 0.33 | 1.1 | 4.8 | 3.8 | 1.7 | 70 | 0.013 | |
| beagle dog | 0.26 | 1.6 | 5.2 | 8.1 | 1.0 | 96 | 0.038 | |
| monkey | 0.61 | 2.2 | 7.7 | 6.1 | 1.7 | 101 | 0.054 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[1]
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Dosage:10 mg/kg
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Administration:Oral gavage
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Result:Significantly decreased Aβ40 levels in the CSF at the 4 h time point at 69%, produced a robust response in the brain with 48% reduction of Aβ40 levels.
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Animal Model:Rats, beagle dog, monkey[1]
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Dosage:2, 5 mg/kg
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Administration:I.v. for 2 mg/kg or p.o. for 5 mg/kg
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Result:Showed moderate total clearance, moderate Vdss, and half-lives of ca. 5-8 h across all three species, and bioavailability was high (70–101%).
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Animal Model:Rats[1]
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Dosage:30 mg/kg
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Administration:P.o.
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Result:Demonstrated dose-dependent decreases in both CSF and brain Aβ levels at 4 h and 8 h time points.
化学情報
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CAS 番号 1215868-94-2
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分子量 442.44
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分子式 C25H19FN4O3
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SMILES
NC(OC1)=N[C@]1(C2=CC(C#CC3(C)COC3)=CN=C2O4)C5=C4C=CC(C6=CC=CN=C6F)=C5
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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)
AMG-8718 関連分類
HY-12938 関連分類
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