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3-Hydroxy desloratadine

Cat. No. M43109
3-Hydroxy desloratadine Structure
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Quality Control & Documentation
Biological Activity

3-Hydroxy desloratidine is a metabolite of Desloratidine.

Chemical Information
Molecular Weight 326.82
Formula C19H19ClN2O
CAS Number 119410-08-1
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] Silvi A Chacko et al. Xenobiotica. Hepatocyte spheroids as a viable in vitro model for recapitulation of complex in vivo metabolism pathways of loratadine in humans

[2] M Keerthana et al. J Biosci. Screening and evaluation of fungal resources for loratadine metabolites

[3] Samir K Gupta et al. J Clin Pharmacol. Multiple-dose pharmacokinetics and safety of desloratadine in subjects with moderate hepatic impairment

[4] Melton Affrime et al. Clin Pharmacokinet. Effect of race and sex on single and multiple dose pharmacokinetics of desloratadine

[5] Melton Affrime et al. Clin Pharmacokinet. A pharmacokinetic profile of desloratadine in healthy adults, including elderly

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