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Kinetics & Metabolic Stability

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Metabolic stability helps evaluate pharmacokinetic parameters, which are essential for determining drug dosing and frequency. 

By understanding how a drug is metabolized, it can be optimized with favorable pharmacokinetic properties.

  • Metabolic stability in hepatocytes, liver microsomes and other subcellular fractions/tissues of interest 
  • Intrinsic clearance in recombinant enzymes, liver microsomes and hepatocytes using the parent depletion method 
  • Vmax and Km determination 

Michaels-Menten Kinetics of Metabolite Formation in Human Hepatocytes

Replicate #​ Vmax​ (pmol/min/million cells)​ Km​ (μM)​ CLint​ (μL/min/million cells)​ 
1​ 143.2​ 16.19​ 8.845​ 
2​ 141.8​ 15.37​ 9.226​ 
3​ 143.8​ 16.53​ 8.699​ 
Mean ± SD​ 142.9 ± 1.03​ 16.02 ± 0.60​ 8.923 ± 0.272​ 

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