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Levofloxacin N-oxide

Cat. No. M39072
Levofloxacin N-oxide Structure
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Biological Activity

Levofloxacin N-oxide is a minor metabolite of Levofloxacin. Levofloxacin N-oxide does not exhibit significantly genotoxic risks. Levofloxacin is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria.

Chemical Information
Molecular Weight 377.37
Formula C18H20FN3O5
CAS Number 117678-38-3
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] Viviane Lucia Beraldo-Araújo et al. Int J Pharm. Levofloxacin in nanostructured lipid carriers: Preformulation and critical process parameters for a highly incorporated formulation

[2] Andrzej Czyrski et al. Sci Rep. The degradation of levofloxacin in infusions exposed to daylight with an identification of a degradation product with HPLC-MS

[3] Poonam Giri et al. Eur J Drug Metab Pharmacokinet. Evaluation of In Vitro Cytochrome P450 Inhibition and In Vitro Fate of Structurally Diverse N-Oxide Metabolites: Case Studies with Clozapine, Levofloxacin, Roflumilast, Voriconazole and Zopiclone

[4] Qingfen Zhu et al. Toxicol Mech Methods. In silico and in vitro genotoxicity evaluation of levofloxacin n-oxide, an impurity in levofloxacin

[5] A Hemeryck et al. Xenobiotica. Pharmacokinetics, metabolism, excretion and plasma protein binding of 14C-levofloxacin after a single oral administration in the Rhesus monkey

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