The active metabolite of proguanil; formed from proguanil by CYP2C19 and CYP3A in human liver microsomes; an inhibitor of DHFR (Kis = 1.5 and 0.79 nM for the P. falciparum and P. berghei enzymes

Cycloguanil (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
152-53-4
Storage:
-20
UN-No:
Non-Hazardous - /

Cycloguanil is the active metabolite of the antimalarial prodrug proguanil.{54317} Cycloguanil is formed from proguanil by the cytochrome P450 (CYP) isoforms CYP2C19 and CYP3A in human liver microsomes. It is an inhibitor of dihydrofolate reductase (DHFR; Kis = 1.5 and 0.79 nM for the P. falciparum and P. berghei enzymes, respectively).{28280,28278} It is active against ten P. falciparum field isolates (IC50s = 0.12-1,400 µg/ml).{28280} Cycloguanil reduces parasitemia in a mouse model of P. berghei infection (ED50 = 2 mg/kg).{54318} It also reduces parasitemia in a rhesus monkey model of P. cynomolgi infection when administered at a dose of 0.3 mg/kg.{54319}  

 

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Description

The active metabolite of proguanil; formed from proguanil by CYP2C19 and CYP3A in human liver microsomes; an inhibitor of DHFR (Kis = 1.5 and 0.79 nM for the P. falciparum and P. berghei enzymes, respectively); active against ten P. falciparum field isolates (IC50s = 0.12-1,400 µg/ml); reduces parasitemia in a mouse model of P. berghei infection (ED50 = 2 mg/kg); reduces parasitemia in a rhesus monkey model of P. cynomolgi infection at 0.3 mg/kg

Formal name: 1-(4-chlorophenyl)-1,6-dihydro-6,6-dimethyl-1,3,5-triazine-2,4-diamine, monohydrochloride

Synonyms:  Chloroguanide Triazine|NSC 3074

Molecular weight: 288.2

CAS: 152-53-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Antiparasitics|Antiprotozoals||Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Parasitic Diseases|Malaria

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