Naphthoquine phosphate
(Synonyms: 磷酸萘酚喹) 目录号 : GC16090
Naphthoquine phosphate 是一种有效且具有口服活性的抗疟药。
Cas No.:173531-58-3
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.1-5.2 nM for various P. falciparum strains [1]
Malaria remains a disease of devastating global impact, killing more than 800,000 people every year-the vast majority being children under the age of 5. Naphthoquine phosphate is a antimalarial drug developed in China.
In vitro: Naphthoquine phosphate showed promising antimalaria acitivities against various P. falciparum strains. Moreover, previoius study highlighted that naphthoquine did not lose potency when tested against chloroquine resistant strains [1].
In vivo: In an study aiming to investigate the antimalarial activity of naphthoquine phosphate combined with artemisinine against Plasmodium knowlesi in rhesus monkey, it was found that the combination of naphthoquine phosphate and artemisinine was superior to the single component and the optimum proportion in the combination is 1 : 2.5 in treating P. knowlesi infection in monkeys [2].
Clinical trial: An oral single dose of the combination drug (400 mg of naphthoquine + 1000mg artemisinin) was administered to adult uncomplicated falciparum malaria patients. Mean fever clearance time, parasite clearance time were 18.2 ± 8.6 h and 34.6 ± 14.3 h, respectively. Adequate clinical and parasitological response was achieved in 52 out of 54 cases, the rate being 98.1%. The drug was well tolerated and no adverse reactionswere detected in the patients [3].
References:
[1] Delves M, Plouffe D, Scheurer C, Meister S, Wittlin S, Winzeler EA, Sinden RE, Leroy D. The activities of current antimalarial drugs on the life cycle stages of Plasmodium: a comparative study with human and rodent parasites. PLoS Med. 2012;9(2):e1001169.
[2] Wang JY, Ding DB, Li GF, Zhao JH. Therapeutic efficacy of naphthoquine phosphate combined with artemisinine against Plasmodium knowlesi. Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 2008;26(6):442-4.
[3] Tun T, Tint HS, Lin K, Kyaw TT, Myint MK, Khaing W, Tun ZW. Efficacy of oral single dose therapy with artemisinin-naphthoquine phosphate in uncomplicated falciparum malaria. Acta Trop. 2009;111(3):275-8.
| Cas No. | 173531-58-3 | SDF | |
| 别名 | 磷酸萘酚喹 | ||
| 化学名 | 2-[(tert-butylamino)methyl]-4-[(7-chloroquinolin-4-yl)amino]-5,6,7,8-tetrahydronaphthalen-1-ol;phosphoric acid | ||
| Canonical SMILES | CC(C)(C)NCC1=CC(=C2CCCCC2=C1O)NC3=C4C=CC(=CC4=NC=C3)Cl.OP(=O)(O)O.OP(=O)(O)O | ||
| 分子式 | C24H34ClN3O9P2 | 分子量 | 605.94 |
| 溶解度 | H2O : 3.33 mg/mL (5.50 mM; Need ultrasonic); DMSO : < 1 mg/mL (insoluble or slightly soluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6503 mL | 8.2516 mL | 16.5033 mL |
| 5 mM | 0.3301 mL | 1.6503 mL | 3.3007 mL |
| 10 mM | 0.165 mL | 0.8252 mL | 1.6503 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet