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Proguanil

Cat. No. M20554
Proguanil Structure
Synonym:

chlorguanide, chloroguanide

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Quality Control & Documentation
Biological Activity

Proguanil is a prophylactic antimalarial drug. It inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell multiplication.

Chemical Information
Molecular Weight 253.73
Formula C11H16ClN5
CAS Number 500-92-5
Solubility (25°C) DMSO 51 mg/mL
Water 1 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Gerlinde F Plger, et al. J Pharm Sci. Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Proguanil Hydrochloride

[2] Samir N Patel, et al. Expert Rev Anti Infect Ther. Atovaquone/proguanil for the prophylaxis and treatment of malaria

[3] Fawziah Marra, et al. Ann Pharmacother. Atovaquone-proguanil for prophylaxis and treatment of malaria

[4] Kate McKeage, et al. Drugs. Atovaquone/proguanil: a review of its use for the prophylaxis of Plasmodium falciparum malaria

[5] A F Fleming. Lancet. Proguanil

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Keywords: Proguanil, chlorguanide, chloroguanide supplier, Anti-infection, inhibitors, activators


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