Hot Sale 58-14-0 price Pyrimethamine supplier CAS NO.58-14-0

Pyrimethamine is an antiprotozoal agent that is primarily active against P. falciparum, inhibiting the protozoal enzyme dihydrofolate reductase (DHFR). By blocking DHFR activity, pyrimethamine prevents the production of tetrahydrofolic acid, an essential coenzyme involved in DNA and RNA synthesis. In in vivo antimalarial mouse models, pyrimethamine displays a prophylactic effect at an ED₅₀ value of 0.5 mg/kg. Sulphonamides act synergistically with pyrimethamine by arresting production of dihydrofolic acid, resulting in the sequential blockade of the folate pathway of protozoa. Pyrimethamine has also been found to limit the expression of the superoxide dismutase 1 (SOD1) gene, a metalloenzyme involved in amyotrophic lateral sclerosis.

Pyrimethamine is a potent inhibitor of multi-drug and toxin extrusion transporters. This compound inhibits Mdr-1(P-glycoprotein) and thus allows for active drugs to stay within the cell for longer periods of time, increasing their effectiveness by preventing efflux of the active compound from the cytoplasm. Pyrimethamine also inhibits DHFR(dihydrofolate reductase ).

Pyrimethamine is a potent inhibitor of multidrug and toxin extrusion (MATE) transporters (K_i values are 46 and 77 nM for human MATE2-K-HEK293 and MATE1-HEK293 cells respectively). Also inhibits dihydrofolate reductase (DHFR) and STAT3. Decreases proliferation of human autosomal dominant polycystic kidney disease cells.

Pyrimethamine is known as an antagonist of folic acid and has an anti-malarial effect. It inhibits dihydrofolate reductase of bacteria and protozoa and affects cell division by inhibiting the conversion of dihydrofolic acid to tetrahydrofolic acid. Its inhibitory effect against human’s dihydrofolate reductase is only 1/1000 in comparison to that of bacteria or protozoa, so that it is considered to be less effective for human