Pyrimethamine

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.Formal Name: 5,4-chlorophenyl-6-ethyl-2,4-pyrimidinediamine. CAS Number: 58-14-0. Synonyms: Darapram, Daraprim(R), Khloridin, NSC 3061. Molecular Formula: C12H13ClN4. Formula Weight: 248.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2.5 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 285 nm. SMILES: ClC1=CC=C(C2=C(CC)N=C(N)N=C2N)C=C1. InChi Code: InChI=1S/C12H13ClN4/c1-2-9-10(11(14)17-12(15)16-9)7-3-5-8(13)6-4-7/h3-6H,2H2,1H3,(H4,14,15,16,17). InChi Key: WKSAUQYGYAYLPV-UHFFFAOYSA-N.