| 货号 | 16861-5mg |
| 描述 | Proguanil is an antimalarial compound used in combination therapy against Plasmodiuminfections.1 Cycloguanil is an active metabolite of proguanil, produced by the cytochrome P450 2C19 isoform.2 It acts as an inhibitor of dihydrofolate reductase (DHFR) (Kis = 0.3 and 1.5 nM for Plasmodium and human forms, respectively).3,4,5 By blocking DHFR activity, cycloguanil prevents the production of tetrahydrofolic acid, an essential coenzyme involved in DNA and RNA synthesis. |
| 别名 | Chloroguanide Triazine;NSC 3074; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Askling, H.H.,Bruneel, F.,Burchard, G., et al. Management of imported malaria in Europe. Malar.J. 11, 1-15 (2012). 2.Wright, J.D.,Helsby, N.A., and Ward, S.A. The role of S-mephenytoin hydroxylase (CYP2C19) in the metabolism of the antimalarial biguanides. British Journal of Clinical Pharmacology 39(4), 441-444 (1995). 3.Foote, S.J.,Galatis, D., and Cowman, A.F. Amino acids in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum involved in cycloguanil resistance differ from those involved in pyrimethamine resistance. Proceedings of the National Academy of Sciences of the United States of America 87(8), 3014-3017 (1990). 4.Yuvaniyama, J.,Chitnumsub, P.,Kamchonwongpaisan, S., et al. Insights into antifolate resistance from malarial DHFR-TS structures. Nature Structural Biology 10, 357-365 (2003). 5.Yuthavong, Y.,Vilaivan, T.,Chareonsethakul, N., et al. Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil-resistant strain (T9/94) of Plasmodium falciparum. Journal of Medicinal Chemistry 43(14), 2738-2744 (2000). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 288.2 |
| 分子式 | C11H14ClN5 • HCl |
| CAS号 | 152-53-4 |
| 稳定性 | ≥ 2 years |
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