NS-181
NS-181 is an orally active MetAP2 inhibitor and antiamebic agent with oral effectiveness.NS-181 functionally inhibits methionine aminopeptidase 2, a protein critical for Entamoeba histolytica proliferation. NS-181 exerts antiamebic activity against Entamoeba histolytica, leading to resolution of amebic liver abscess. NS-181 can be used for the research of amebiasis.
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: 3075693-63-6
- 分子式: C24H28O7
- 分子量:428.47
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
NS-181 (30 min) resists hamster liver microsome-mediated metabolism and retains potent antiamebic activity (ED50 of 14.6 nM) after 30 min of microsomal incubation[1].
NS-181 (10 μM) exhibits no cytotoxicity against Huh-7 human hepatocellular carcinoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:unstated specific strain[1]
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Dosage:15 mg/kg (subcutaneous); 30 mg/kg (oral)
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Administration:s.c.; 5 consecutive days; p.o.; 5 consecutive days
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Result:Achieved complete resolution of amebic liver abscess, with abscess weight proportion relative to whole liver reduced to near 0%, amebic mRNA levels in liver reduced, and inflammation levels decreased to match noninfected controls.
Significantly reduced amebic liver abscess size, with abscess weight proportion relative to whole liver markedly decreased compared to vehicle controls.
化学情報
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CAS 番号 3075693-63-6
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分子量 428.47
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分子式 C24H28O7
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SMILES
O=C(O[C@H](C(CC1)=O)[C@@]([C@@]2(C)O[C@@H]2C/C=C(C)\C)(O)[C@]31CO3)/C=C/C4=CC=CC(O)=C4
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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)