Antimalarial agent 52
Antimalarial agent 52 is an orally active formation of synthetic hemozoin (β-hematin) inhibitor with an IC50 of 6.6 μM. Antimalarial agent 52 exhibits in vitro antiplasmodial activity against P. falciparum Pf3D7, PfDd2 strains and P. knowlesi with IC50s of 6.1, 6.4 and 3.3 nM. Antimalarial agent 52 remain highly effective against multidrug-resistant strains and demonstrates curative activity in the P. berghei mouse model.
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: C24H17BrClF5N2O
- 分子量:559.75
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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
製品説明
体外実験
Antimalarial agent 52 (Compound 7d) (48 h) exhibits antiplasmodial activity against field isolates from malaria patients and drug-resistant mutant strains with IC50s of 4-16 nM and 8-15 nM[1].
Antimalarial agent 52 is not metabolized by human liver microsomes, has high plasma stability and shows improved cardiac safety[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | AUC0-t | Brain-to-Plasma Ratio |
|---|---|---|---|---|---|---|
| Mice[1] | 50 mg/kg | p.o. | 2236.4 ng/mL | 49002 ng·h/mL | 4 h | 0.97 |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:P. berghei infection model established in female NMRI mice[1]
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Dosage:3, 10, 30 and 50 mg/kg
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Administration:Oral administration (p.o.), 4, 24, 48, 72 hours after infection for 4 doses
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Result:Showed significant dose-dependent antimalarial activity.
化学情報
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分子量 559.75
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分子式 C24H17BrClF5N2O
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SMILES
N=C(NC1=CC=C(Br)C=C1)CC(C2=CC3=C(F)C=C(F)C=C3C4=CC(C(F)(F)F)=CC=C42)O.Cl
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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)