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Cycloguanil

Cat. No. M30226
Cycloguanil Structure
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Quality Control & Documentation
Biological Activity

Cycloguanil, the active metabolite of Proguanil, acts on malaria schizonts in erythrocytes and hepatocytes.

Chemical Information
Molecular Weight 251.72
Formula C11H14ClN5
CAS Number 516-21-2
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jennifer I Brown, et al. Metabolites. Cycloguanil and Analogues Potently Target DHFR in Cancer Cells to Elicit Anti-Cancer Activity

[2] Giusy Tassone, et al. Pharmaceuticals (Basel). Evidence of Pyrimethamine and Cycloguanil Analogues as Dual Inhibitors of Trypanosoma brucei Pteridine Reductase and Dihydrofolate Reductase

[3] Giacomo Landi, et al. ACS Infect Dis. Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors

[4] Maarten van der Velden, et al. Malar J. Proguanil and cycloguanil are organic cation transporter and multidrug and toxin extrusion substrates

[5] E Petersen, et al. Ann Trop Med Parasitol. In vitro and in vivo susceptibility of Plasmodium falciparum isolates from Liberia to pyrimethamine, cycloguanil and chlorcycloguanil

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