A prodrug form of cycloguanil; metabolized by CYP2C19 and CYP3A to form cycloguanil in human liver microsomes; active against chloroquine- and quinine-resistant strains of P. falciparum alone or in combination with atovaquone (EC50s = 0.22-2.67 and 0.37-1.6 µM

Proguanil – 10 mg

Brand:
Cayman
CAS:
500-92-5
Storage:
-20
UN-No:
Non-Hazardous - /

Proguanil is a prodrug form of the antimalarial agent cycloguanil (Item No. 16861).{54317} 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 (Item No. 23802) with EC50 values ranging from 0.22 to 2.67 and 0.37 to 1.6 µM, respectively.{52699} It reduces parasitemia in a mouse model of P. berghei infection with a minimum effective dose (MED) of 32 mg/kg.{52700} Formulations containing proguanil have been used in combination with atovaquone for the prevention and treatment of malaria.  

 

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Description

A prodrug form of cycloguanil; metabolized by CYP2C19 and CYP3A to form cycloguanil in human liver microsomes; active against chloroquine- and quinine-resistant strains of P. falciparum alone or in combination with atovaquone (EC50s = 0.22-2.67 and 0.37-1.6 µM, respectively); reduces parasitemia in a mouse model of P. berghei infection (MED = 32 mg/kg)

Formal name: N-(4-chlorophenyl)-N′-(1-methylethyl)-imidodicarbonimidic diamide

Synonyms:  Chlorguanide|Chloroguanide

Molecular weight: 253.7

CAS: 500-92-5

Purity: ≥98%

Formulation: A solid

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