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4-Hydroxy Atorvastatin lactone

Cat. No. M42338
4-Hydroxy Atorvastatin lactone Structure
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Biological Activity

4-Hydroxy Atorvastatin lactone is a metabolite of Atorvastatin.

Chemical Information
Molecular Weight 556.62
Formula C33H33FN2O5
CAS Number 163217-70-7
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] Anne M Filppula et al. Drug Metab Dispos. Comparative Hepatic and Intestinal Metabolism and Pharmacodynamics of Statins

[2] Lloyd R Whitfield et al. J Clin Pharmacol. Effect of gemfibrozil and fenofibrate on the pharmacokinetics of atorvastatin

[3] Y Y Lau et al. Clin Pharmacol Ther. effect of OATP1B transporter inhibition on the pharmacokinetics of atorvastatin in healthy volunteers

[4] M Jemal et al. Rapid Commun Mass Spectrom. Quantitation of the acid and lactone forms of atorvastatin and its biotransformation products in human serum by high-performance liquid chromatography with electrospray tandem mass spectrometry

[5] T Kantola et al. Clin Pharmacol Ther. Effect of itraconazole on the pharmacokinetics of atorvastatin

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