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Catalog No.S2006

5 publications

Pyrimethamine Chemical Structure

CAS No. 58-14-0

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

Selleck's Pyrimethamine has been cited by 5 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]


Solubility (25°C)

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

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Chemical Information

Molecular Weight 248.71


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

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DHFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID