Pyrimethamine

Catalog No.S2006

Pyrimethamine Chemical Structure

Molecular Weight(MW): 248.71

Pyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 310 In stock
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Biological Activity

Description Pyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.
Targets
DHFR [1]
15.4 nM
In vitro

Pyrimethamine has an IC50 of 5–13 μM for the Hex isozymes at pH 4.3. Pyrimethamine increases the enzyme activity and protein level of the α and β subunits of Hex A in the βR505Q/Δ16kb cell line. [1] Pyrimethamine-sulfadoxine is an inhibitor of dihydrofolate reductase(DHFR) that has been widely used to treat chloroquine-resistant Plasmodium falciparum malaria. [2] Pyrimethamine is a potent inhibitor of mouse (m)Mate1 (K(i) = 145 nM) among renal organic cation transporters mOctn1 and mOctn2 (K(i) > 30 mM), mOct1 (K(i) = 3.6 mM), and mOct2 (K(i) = 6.0 mM). Pyrimethamine inhibits the uptake of metformin by kidney brush-border membrane vesicles (BBMVs) (K(i) = 41 nM) and canalicular membrane vesicles in the presence of outward gradient of H+. Pyrimethamine treatment significantly increases the kidney-to-plasma ratio of tetraethylammonium, and both the liver- and kidney-to-plasma ratios of metformin in mice, whereas it does not affect their plasma concentrations and urinary excretion rates. Pyrimethamine is a potent inhibitor of human (h)MATE1 and hMATE2-K (K(i) = 77 and 46 nM, respectively) and H+ and organic cation exchanger in human kidney BBMVs (K(i) = 31 nM) in the presence of outward gradient of H+. [3]

Protocol

Solubility (25°C)

In vitro DMSO 10 mg/mL (40.2 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 248.71
Formula

C12H13ClN4

CAS No. 58-14-0
Storage powder
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02511054 Completed Malaria National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) July 21, 2015 Phase 1
NCT03009526 Not yet recruiting Malaria|Pregnancy University of Malawi College of Medicine|Centers for Disease Control and Prevention January 2017 Phase 3
NCT02909712 Recruiting Malaria|Pregnancy|Cardiotoxicity|Parasitemia London School of Hygiene and Tropical Medicine|Kilimanjaro Christian Medical Centre, Tanzania|National Institute for Medical Research, Tanzania September 2016 Phase 2
NCT02793622 Recruiting Malaria University of California, San Francisco|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|Bill and Melinda Gates Foundation September 2016 Phase 3
NCT02831023 Completed Malaria University of California, San Francisco|Malaria Research and Training Center, Bamako, Mali|Radboud University|London School of Hygiene and Tropical Medicine|Heidelberg University|Bill and Melinda Gates Foundation July 2016 Phase 2
NCT02836002 Recruiting Malaria Radboud University|The PATH Malaria Vaccine Initiative (MVI)|QIMR Berghofer Medical Research Institute June 2016 Phase 1|Phase 2

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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.

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DHFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID