Antimalarial agent 55
Antimalarial agent 55 is an orally potent inhibitor of PfA-M1 and PfA-M17 aminopeptidases from Plasmodium falciparum, with Ki values of 27 nM and 81 nM, respectively. Antimalarial agent 55 exhibits potent nanomolar activity against homologous enzymes from Plasmodium vivax and Plasmodium berghei, with Ki values of 2 nM, 4 nM, 190 nM and 18 nM for Pv-M1, Pb-M1, Pv-M17 and Pb-M17, respectively. Antimalarial agent 55 possesses significant antiplasmodial activity, as well as cross-species inhibitory capacity and broad-spectrum activity that is unaffected by existing drug resistance mechanisms. Antimalarial agent 55 can be used in malaria 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: C17H21N3O3
- 分子量:315.37
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
Antimalarial agent 55 (Compound 3k) (72 h) exhibits in vitro killing activity against the Plasmodium falciparum strain Pf3D7, with an EC50 of 31 nM; it also shows potent activity against clinically isolated Plasmodium falciparum strains with different drug resistance mechanisms.
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:Arc:Arc(Swiss) (female, 6-weeks of age, intraperitoneal infection with 2 × 107 Plasmodium berghei ANKA-infected erythrocytes)[1]
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Dosage:50 mg/kg
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Administration:p.o.; at 2 h, day 1, day 2, and day 3 postinfection
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Result:Achieved 100% antimalarial activity at 3 days post-infection.\nAchieved 83% antimalarial activity at 4 days post-infection.\nAchieved 63% antimalarial activity at 6 days post-infection.
化学情報
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分子量 315.37
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分子式 C17H21N3O3
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SMILES
CC(C)(C)CC(NC(C1=CC=C2C=CC=NC2=C1)C(NO)=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)
- Antimalarial agent 55
- Antimalarial agent55
- Antimalarial agent-55
- Parasite
- Aminopeptidase
- Plasmodium falciparum M17
- Plasmodium berghei M17
- Plasmodium berghei M1
- Plasmodium aminopeptidase
- Plasmodium falciparum M1
- human embryonic kidney cells
- Plasmodium vivax M17
- Plasmodium vivax M1
- Plasmodium falciparum strains
- human cytochrome P450 isoforms
- Inhibitor
- inhibitor
- inhibit