Home Metabolism DHFR inhibitor Pyrimethamine For research use only.

Pyrimethamine

Synonyms: RP 4753

Pyrimethamine(RP 4753) is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.

Pyrimethamine Chemical Structure

Pyrimethamine Chemical Structure

CAS: 58-14-0

Selleck's Pyrimethamine has been cited by 9 publications

Purity & Quality Control

Batch: Purity: 100%
100

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Biological Activity

Description Pyrimethamine(RP 4753) is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.
Targets
DHFR [1]
15.4 nM
In vitro
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05678348 Recruiting Head and Neck Cancer|Cancer of the Head and Neck Washington University School of Medicine|Vyera Pharmaceuticals August 3 2023 Early Phase 1
NCT06162078 Recruiting Maternal Malaria During Pregnancy - Baby Not Yet Delivered Groupe de Recherche Action en Sante August 25 2023 --
NCT05979896 Recruiting Malaria Malaria Consortium July 28 2023 Phase 4
NCT05478954 Active not recruiting Malaria Malaria Consortium July 15 2022 Phase 4
NCT05471544 Active not recruiting Malaria Malaria Consortium July 18 2022 Phase 3

Chemical lnformation & Solubility

Molecular Weight 248.71 Formula

C12H13ClN4

CAS No. 58-14-0 SDF Download Pyrimethamine SDF
Smiles CCC1=C(C(=NC(=N1)N)N)C2=CC=C(C=C2)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 10 mg/mL ( (40.2 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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