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Naphthoquine phosphate

Catalog No.
A3641
Antimalarial drug
Grouped product items
SizePriceStock Qty
5mg
$38.00
In stock
10mg
$61.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Background

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.

Chemical Properties

StorageStore at -20°C
M.Wt605.94
Cas No.173531-58-3
FormulaC24H34ClN3O9P2
SolubilitySoluble in DMSO
Chemical Name2-[(tert-butylamino)methyl]-4-[(7-chloroquinolin-4-yl)amino]-5,6,7,8-tetrahydronaphthalen-1-ol;phosphoric acid
SDFDownload SDF
Canonical SMILESCC(C)(C)NCC1=CC(=C2CCCCC2=C1O)NC3=C4C=CC(=CC4=NC=C3)Cl.OP(=O)(O)O.OP(=O)(O)O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment [1]:

Model organism

Plasmodium falciparum

Preparation method

The solubility of this compound in DMSO is soluble. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10μM

Applications

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

Animal experiment [1]:

Animal models

Monkey model of Plasmodium Knowles infection

Dosage form

6 or 10 mg/kg (i.g.), once a day for 3 days

Application

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.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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 Feb;9(2): e 1001169. doi: 10.1371/journal.pmed.1001169. Epub 2012 Feb 21. PubMedPMID: 22363211; PubMed Central PMCID: PMC3283556.

[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 Dec 30;26(6):442-4. Chinese.PubMed PMID: 19288919.

Biological Activity

Description Naphthoquine phosphate is an antimalarial drug.
Targets malaria          
IC50            

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

Naphthoquine phosphate