Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 1-(4-chlorophenyl)-1,6-dihydro-6,6-dimethyl-d3-1,3,5-triazine-2,4-diamine, monohydrochloride
Purity: ≥99% deuterated forms (d1-d6)
Formula Markup: C11H8ClD6N5 / HCl
Formula Weight: 294.21226
CAS Number: 2712364-69-5
Notes: Cycloguanil-d6 is intended for use as an internal standard for the quantification of cycloguanil (Item No. 16861) by GC- or LC-MS. 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}