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

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Control de calidad (Quality Control)

Lote: Pureza: 99.77%

99.77

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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	455.34	Fórmula	C₁₅H₂₁N₃O.2H₃O₄P	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	63-45-6	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	N/A			Smiles	CC(CCCN)NC1=C2C(=CC(=C1)OC)C=CC=N2.OP(=O)(O)O.OP(=O)(O)O

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 91 mg/mL (199.85 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : 91 mg/mL

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	4.550mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 91 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	0.750mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

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.

Referencias

[1] https://pubmed.ncbi.nlm.nih.gov/18930565/

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Primaquine Diphosphate Anti-infection chemical

Estructura química

Peso molecular: 455.34