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Primaquine Diphosphate

Name: Primaquine Diphosphate
Brand: Selleck Chemicals
SKU: S4237
Rating: 5 (3 reviews)

Catalog No.S4237 Purity:99.8%

Primaquine Diphosphate is a transmission-blocking anti-malarial clinically available, displaying a marked activity against gametocytes of all species of human malaria.

Primaquine Diphosphate Chemical Structure

CAS No. 63-45-6

Purity & Quality Control

Batch: Purity: 99.8%

99.8

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Biological Activity

Description	Primaquine Diphosphate is a transmission-blocking anti-malarial clinically available, displaying a marked activity against gametocytes of all species of human malaria.

In vitro
In vitro	Primaquine is still the only transmission-blocking anti-malarial clinically available, displaying a marked activity against gametocytes of all species of human malaria, including multi-resistant Plasmodium falciparum strains. Primaquine is also effective against all exoerythrocytic forms of the parasite and is used in conjunction with other anti-malarials for the treatment of vivax and ovale malaria. The exact mechanism by which Primaquine so effectively eliminates Plasmodium falciparum and gametocytes is still unknown, but it is thought that metabolism at the parasites’ mitochondria is impaired, eventually by interference with the ubiquinone function as an electron carrier in the respiratory chain. Another potential mechanism of anti-malarial action by Primaquine is the production of highly reactive metabolites that generate intracellular oxidative potentials. Primaquine is found to be an inhibitor of vesicular transport and blocks the calcium-release-activated current in rat megakaryocytes. Primaquine also acts on cardiac Na⁺ channels in isolated rat ventricular muscle and myocytes. Primaquine inhibits protein transport with IC50 of 50 μM, and inhibits the budding of vesicles from the donor membranes. PQ has a strong inhibitory effect on the recycling of endocytosed proteins to the plasma membrane. Primaquine is able to inhibit the potassium current by blockade of muscarinic receptors. Primaquine also inhibit human erythrocyte membrane acetylcholinesterase (AChE) with IC33 of 30 μM. Primaquine is a nitrite-reacting mutagen precursor where the secondary amino group plays a key role. ^[1]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05879224	Recruiting	Vivax Malaria\|G6PD Deficiency	Menzies School of Health Research\|Gadjah Mada University\|Universitas Sumatera Utara\|Indonesia University\|Yayasan Pengembangan Kesehatan dan Masyarakat\|Indonesian National Malaria Control Program Ministry of Health\|National Research and Innovation Agency of Indonesia\|Burnet Institute\|University of Melbourne\|Medicines for Malaria Venture\|PATH\|UNITAID\|Institute of Tropical Medicine Belgium	August 7 2023	Not Applicable
NCT04984759	Withdrawn	Healthy Lactating Women	University of Oxford\|Mahidol Oxford Tropical Medicine Research Unit	July 1 2023	Phase 4
NCT05874271	Recruiting	Vivax Malaria\|G6PD Deficiency	Macfarlane Burnet Institute for Medical Research and Public Health Ltd\|Papua New Guinea Institute of Medical Research\|Papua New Guinea National Department of Health\|Menzies School of Health Research\|University of Melbourne\|Medicines for Malaria Venture\|PATH\|UNITAID	July 10 2023	Not Applicable
NCT05044637	Recruiting	Malaria Vivax	Fundação de Medicina Tropical Dr. Heitor Vieira Dourado\|Bill and Melinda Gates Foundation\|Conselho Nacional de Desenvolvimento Científico e Tecnológico	August 26 2021	Phase 2
NCT04073953	Unknown status	G6PD Deficiency	University of Mississippi Oxford\|University of Colorado Denver\|Southern Research Institute	September 1 2020	Phase 1

References

[1] Vale N, et al. Eur J Med Chem, 2009, 44(3), 937-953.

Chemical Information & Solubility

Molecular Weight	455.34	Formula	C₁₅H₂₁N₃O.2H₃O₄P
CAS No.	63-45-6	SDF	Download Primaquine Diphosphate SDF
Smiles	CC(CCCN)NC1=C2C(=CC(=C1)OC)C=CC=N2.OP(=O)(O)O.OP(=O)(O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 91 mg/mL ( (199.85 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 91 mg/mL

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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