product name Pyrimethamine
Description: Pyrimethamine is a dihydrofolate reductase (DHFR) inhibitor which is used as an antimalarial and antiprotozoal drug. Pyrimethamine prevents the production of tetrahydrofolic acid, an essential coenzyme involved in DNA and RNA synthesis. Pyrimethamine has also been found to limit the expression of the superoxide dismutase 1 gene, a protein involved in amyotrophic lateral sclerosis.
References: J Biol Chem. 2007 Mar 23;282(12):9150-61; J Am Coll Cardiol. 2002 Aug 21;40(4):803-10.
248.71
Formula
C12H13ClN4
CAS No.
58-14-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 10 mg/mL (40.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19410549
| In Vitro |
In vitro activity: 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. Pyrimethamine-sulfadoxine is an inhibitor of dihydrofolate reductase(DHFR) that has been widely used to treat chloroquine-resistant Plasmodium falciparum malaria. 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+. Kinase Assay: Cell Assay: |
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| In Vivo | |
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| Formulation & Dosage | |
| References | J Biol Chem. 2007 Mar 23;282(12):9150-61; J Am Coll Cardiol. 2002 Aug 21;40(4):803-10. |
