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Primaquine diphosphate

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Catalog No. T0850Cas No. 63-45-6
Alias Primaquine phosphate, Primaquine bisphosphate

Primaquine diphosphate is the phosphate salt form of primaquine, a synthetic, 8-aminoquinoline derivative with antimalarial properties. Although its mechanism of action is unclear, primaquine bind to and alter the properties of protozoal DNA. This agent eliminates tissue (exo-erythrocytic) malarial infection, preventing the development of the erythrocytic forms of the parasite which are responsible for relapses in Plasmodium vivax and ovale malaria. Primaquine is active against late hepatic stages (hypnozoites, schizonts).

Primaquine diphosphate

Primaquine diphosphate

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Purity: 99.82%
Catalog No. T0850Alias Primaquine phosphate, Primaquine bisphosphateCas No. 63-45-6
Primaquine diphosphate is the phosphate salt form of primaquine, a synthetic, 8-aminoquinoline derivative with antimalarial properties. Although its mechanism of action is unclear, primaquine bind to and alter the properties of protozoal DNA. This agent eliminates tissue (exo-erythrocytic) malarial infection, preventing the development of the erythrocytic forms of the parasite which are responsible for relapses in Plasmodium vivax and ovale malaria. Primaquine is active against late hepatic stages (hypnozoites, schizonts).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 g$40-In Stock
2 g$51-In Stock
1 mL x 10 mM (in DMSO)$29In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.82%
Color:Orange to Red
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Product Introduction

Bioactivity
Description
Primaquine diphosphate is the phosphate salt form of primaquine, a synthetic, 8-aminoquinoline derivative with antimalarial properties. Although its mechanism of action is unclear, primaquine bind to and alter the properties of protozoal DNA. This agent eliminates tissue (exo-erythrocytic) malarial infection, preventing the development of the erythrocytic forms of the parasite which are responsible for relapses in Plasmodium vivax and ovale malaria. Primaquine is active against late hepatic stages (hypnozoites, schizonts).
In vivo
Primaquine effectively counters all exoerythrocytic forms of parasites and is used in conjunction with other antimalarial drugs to treat vivax and ovale malaria. It remains an efficacious malaria-blocking agent, exhibiting notable activity against the gametocytes of all human malaria, including multidrug-resistant strains of P. falciparum. The specific mechanism by which Primaquine eliminates P. falciparum and gametocytes is unclear, but studies suggest it involves disruptions to the parasite's mitochondrial metabolism, impairing coenzyme Q's role as an electron carrier in the respiratory chain, and potential generation of highly reactive metabolites leading to increased oxidative potential. Primaquine can block calcium-release-activated channels in rat megakaryocytes and may also act as an inhibitor of vesicular transport. It inhibits protein transport (IC50: 50 μM) and vesicle budding in donor cell membranes. Primaquine significantly suppresses the recycling of phagocytosed proteins to the plasma membrane and inhibits potassium channel currents by blocking muscarinic acetylcholine receptors. It also inhibits human erythrocyte membrane acetylcholinesterase (IC33: 30 μM) and affects the sodium channels in isolated rat ventricular muscle and myocytes.
SynonymsPrimaquine phosphate, Primaquine bisphosphate
Chemical Properties
Molecular Weight455.34
FormulaC15H21N3O·2H3PO4
Cas No.63-45-6
SmilesCC(CCCN)Nc1c2c(cc(c1)OC)cccn2.OP(=O)(O)O.OP(=O)(O)O
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 245 mg/mL (538.06 mM), Sonication is recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: 83 mg/mL (182.28 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.39 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM2.1962 mL10.9808 mL21.9616 mL109.8081 mL
5 mM0.4392 mL2.1962 mL4.3923 mL21.9616 mL
10 mM0.2196 mL1.0981 mL2.1962 mL10.9808 mL
20 mM0.1098 mL0.5490 mL1.0981 mL5.4904 mL
50 mM0.0439 mL0.2196 mL0.4392 mL2.1962 mL
100 mM0.0220 mL0.1098 mL0.2196 mL1.0981 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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