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Cycloguanil hydrochloride

Cat. No. M28570
Cycloguanil hydrochloride Structure
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Biological Activity

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

Chemical Information
Molecular Weight 288.18
Formula C11H15Cl2N5
CAS Number 152-53-4
Form Solid
Solubility (25°C) DMSO 62.5 mg/mL (ultrasonic)
Water 25 mg/mL (ultrasonic and warming and heat to 60°C)
Storage 4°C, dry, sealed
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] Giacomo Landi, et al. ACS Infect Dis. Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors

[3] Gerlinde F Plöger, et al. J Pharm Sci. Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Proguanil Hydrochloride

[4] M Pudney, et al. J Travel Med. Atovaquone and proguanil hydrochloride: a review of nonclinical studies

[5] E Holfels, et al. Antimicrob Agents Chemother. In vitro effects of artemisinin ether, cycloguanil hydrochloride (alone and in combination with sulfadiazine), quinine sulfate, mefloquine, primaquine phosphate, trifluoperazine hydrochloride, and verapamil on Toxoplasma gondii

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