Catalog No.S2006

For research use only.

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

Pyrimethamine Chemical Structure

CAS No. 58-14-0

Selleck's Pyrimethamine has been cited by 6 Publications

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Biological Activity

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 248.71


CAS No. 58-14-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=C(C(=NC(=N1)N)N)C2=CC=C(C=C2)Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04577469 Not yet recruiting Drug: Maldox tablets|Drug: G-COSPE® tablets Bioequivalence Emzor Pharmaceutical Industries Limited December 2020 Phase 1
NCT03599596 Unknown status Drug: Sulphadoxine-pyrimethamine Malaria University College Hospital Ibadan September 1 2018 Phase 1
NCT03525730 Completed Drug: Valproic Acid|Drug: Pyrimethamine HIV-1-infection Erasmus Medical Center April 18 2018 Phase 1|Phase 2
NCT03258762 Completed Drug: Pyrimethamine|Drug: Calcium folinate Toxoplasmosis GlaxoSmithKline September 25 2017 Phase 1
NCT02527005 Completed Drug: Sulphadoxine-pyrimethamine|Drug: Azithromycin Malaria|Pregnant|HIV University of Ibadan September 2015 Phase 1

(data from, updated on 2022-01-17)

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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