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Voriconazole N-oxide

Cat. No. M41144
Voriconazole N-oxide Structure
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Biological Activity

Voriconazole N-oxide (Voriconazole oxynitride) is a potent antifungal agent.

Chemical Information
Molecular Weight 365.31
Formula C16H14F3N5O2
CAS Number 618109-05-0
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] Josefine Schulz et al. Pharm Res. Microdialysis of Voriconazole and its N-Oxide Metabolite: Amalgamating Knowledge of Distribution and Metabolism Processes in Humans

[2] Zaiming Liang et al. Front Pharmacol. Inflammation Affects Liver Function and the Metabolism of Voriconazole to Voriconazole-N-Oxide in Adult and Elderly Patients

[3] Yong Yu et al. J Chromatogr Sci. Simultaneous Determination of Voriconazole and Its Voriconazole N-Oxide Metabolite in Human Urine by Liquid Chromatography/Tandem Mass Spectrometry

[4] Shenglan Shang et al. Mycoses. Effect of CYP2C19 polymorphism on the plasma voriconazole concentration and voriconazole-to-voriconazole-N-oxide concentration ratio in elderly patients

[5] K Ona et al. Br J Dermatol. Voriconazole N-oxide and its ultraviolet B photoproduct sensitize keratinocytes to ultraviolet A

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