Proguanil

Proguanil is a prodrug form of the antimalarial agent cycloguanil (Cay-16861). Proguanil is metabolized by the cytochrome P450 (CYP) isoforms CYP2C19 and CYP3A to form cycloguanil in human liver microsomes. It is active against chloroquine- and quinine-resistant strains of P. falciparum alone or in combination with atovaquone (Cay-23802) with EC50 values ranging from 0.22 to 2.67 and 0.37 to 1.6 µM, respectively. It reduces parasitemia in a mouse model of P. berghei infection with a minimum effective dose (MED) of 32 mg/kg. Formulations containing proguanil have been used in combination with atovaquone for the prevention and treatment of malaria.Formal Name: N-(4-chlorophenyl)-N'-(1-methylethyl)-imidodicarbonimidic diamide. CAS Number: 500-92-5. Synonyms: Chlorguanide, Chloroguanide. Molecular Formula: C11H16ClN5. Formula Weight: 253.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 2mg/mL, DMSO: 3mg/mL, DMSO:PBS (pH 7.2) (1:10): 0.09mg/mL, Ethanol: 1mg/mL. lambdamax: 259 nm. SMILES: ClC1=CC=C(NC(NC(NC(C)C)=N)=N)C=C1. InChi Code: InChI=1S/C11H16ClN5/c1-7(2)15-10(13)17-11(14)16-9-5-3-8(12)4-6-9/h3-7H,1-2H3,(H5,13,14,15,16,17). InChi Key: SSOLNOMRVKKSON-UHFFFAOYSA-N.