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N-Desmethyl Sildenafil

Cat. No. M39170
N-Desmethyl Sildenafil Structure
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Quality Control & Documentation
Biological Activity

N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.

Chemical Information
Molecular Weight 460.55
Formula C21H28N6O4S
CAS Number 139755-82-1
Form Solid
Solubility (25°C) DMSO 150 mg/mL (ultrasonic)
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] Wen Ling Zhu et al. J Chromatogr Sci. UPLC-MS/MS for the Simultaneous Determination of Sildenafil and N-Desmethyl Sildenafil

[2] Jie Huang et al. Int J Clin Pharmacol Ther. A UPLC-MS/MS method for simultaneous quantification of sildenafil and N-desmethyl sildenafil applied in pharmacokinetic and bioequivalence studies in a Chinese population

[3] Bianca Maria Goffredo et al. Biomed Chromatogr. Reverse-phase high-performance liquid chromatography for the simultaneous determination of sildenafil and N-desmethyl sildenafil in plasma of children

[4] Kai Bin Liew et al. Biomed Chromatogr. Simultaneous quantification of sildenafil and N-desmethyl sildenafil in human plasma by UFLC coupled with ESI-MS/MS and pharmacokinetic and bioequivalence studies in Malay population

[5] Péter Barabás et al. Neurochem Int. Sildenafil, N-desmethyl-sildenafil and Zaprinast enhance photoreceptor response in the isolated rat retina

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