Antimalarial agent 64
Antimalarial agent 64 is an orally active acridine-based antimalarial derivative and also a rapid-acting inhibitor of hemozoin formation. Antimalarial agent 64 exhibits nanomolar inhibitory activity against field isolates of Plasmodium falciparum and Plasmodium vivax. Antimalarial agent 64 localizes near the digestive vacuole of Plasmodium. Antimalarial agent 64 can be used for the research of malaria.
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- CAS 番号: 2770244-63-6
- 分子式: C26H29ClN4O2
- 分子量:464.99
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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 64 (Compound 2d) potently inhibits Chloroquine (HY-17589A)-sensitive Plasmodium falciparum 3D7 strain growth with an IC50 of 20 nM, has a CC50 of 6 μM against HepG2 cells, and a selectivity index of 300[1].
Antimalarial agent 64 retains potent antiplasmodial activity against Plasmodium falciparum K1, Dd2, and 3D7R_MMV848 multidrug-resistant strains but shows cross-resistance with atovaquone in the TM90C6B strain[1].
Antimalarial agent 64 potently inhibits ex vivo growth of Plasmodium falciparum (IC50 = 39 nM) and Plasmodium vivax (IC50 = 21 nM) field isolates from the Brazilian Amazon[1].
Antimalarial agent 64 potently inhibits ring and trophozoite stages of Plasmodium falciparum 3D7 strain, with reduced activity against schizonts[1].
Antimalarial agent 64 (10 μM) selectively accumulates near the digestive vacuole of Plasmodium falciparum-infected erythrocytes, with no uptake in uninfected red blood 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:
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Dosage:50 mg/kg/day
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Administration:p.o.; once daily; 3 consecutive days post-infection
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Result:Achieved 100% reduction in parasitemia at days 5, 8, and 11 post-infection compared to untreated controls.
Showed 100% survival at 30 days post-infection, comparable to chloroquine-treated controls.
化学情報
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CAS 番号 2770244-63-6
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分子量 464.99
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分子式 C26H29ClN4O2
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SMILES
COC1=CC2=C(C3=CC=C(C=C3N=C2C=C1)Cl)NC4=CC(CN(C)C)=C(C(CN(C)C)=C4)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)