Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Pyrimethamine is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.
Description | Pyrimethamine is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug. |
Targets&IC50 | DHFR: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] |
Synonyms | 乙胺嘧啶, RP 4753, Pirimetamin, Pirimecidan |
Molecular Weight | 248.71 |
Formula | C12H13ClN4 |
CAS No. | 58-14-0 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Ethanol: 2.5 mg/mL (10 mM)
DMSO: 24.9 mg/mL (100 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Pyrimethamine 58-14-0 DNA损伤和修复 代谢 微生物学 细胞周期 Antifolate DHFR Parasite Pirimecidan folic–folinic acid systems Pirimetamin parasites nucleoprotein metabolism RP-4753 inhibit cell division RP4753 RP 4753 Inhibitor antimalarial inhibitor