CAS No.: 1469439-69-7
Cabamiquine Catalog No. CSN24178
Synonyms: DDD107498;DDD-498;M5717
DDD107498 is a multiple-stage antimalarial agent targeting on eEF2.
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纯度 & 质量文件
批次:
靶点选择性
生物活性
- 描述
- 作用机制
动物研究 剂量 Mice: 1 mg/kg[1] (i.v.); 3 mg/kg - 30 mg/kg[1] (p.o.) Rat: 1 mg/kg[1] (i.v.); 5 mg/kg, 10 mg/kg[1] (p.o.)
给药途径 i.v., p.o.
动物药代数据 Animal Mice[2] Rats[2] Dose 3 mg/kg (i.v.)
10 mg/kg (p.o.)1 mg/kg (i.v.)
3 mg/kg (p.o.)Administration i.v.
p.o.i.v.
p.o.F 74% (p.o.) 84% (p.o.) CLb 12 ml/min/kg (i.v.) 18 ml/min/kg (i.v.) T1/2 16 h (i.v.) 10 h (i.v.) Tmax 1 h (p.o.) 4 h (p.o.) Cmax 90 ng/ml (p.o.) 180 ng/ml (p.o.) Vdss 15 L/kg (i.v.) 15 L/kg (i.v.) AUC 179272 ng·min/kg (p.o.) 200542 ng·min/kg (p.o.) - 参考文献
- [1] Baragaña B, Hallyburton I, et al. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015 Jun 18;522(7556):315-20.
- [2] Baragaña B, Norcross NR, et al. Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy. J Med Chem. 2016 Nov 10;59(21):9672-9685. Epub 2016 Sep 10.
- [3] Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Erratum in: Nature. 2016 Sep 1;537(7618):122. PMID: 26085270; PMCID: PMC4700930.
实验方案
- 计算器
- 储存液制备
技术信息
| CAS号 | 1469439-69-7 | 储存条件 |
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| 分子式 | C27H31FN4O2 | 运输 | 蓝冰 | |||||
| 分子量 | 462.56 | 别名 | DDD107498;DDD-498;M5717 | |||||
| 溶解度 |
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动物实验配方 |
