TABLE 1

Incubation conditions for experiments performed in pooled human hepatocytes, human liver microsomes, human S9 fractions, and recombinant P450 enzymes

In Vitro SystemProtein Conc.Fraction UnboundIncubation Time
min
Hepatocytesa0.4b0.8915
HLMa0.3c0.8510
S9a,d1.5c0.5315
rCYP2C8a50e0.8810
rCYP3A4a30e0.9810
rCYP3A5a100e0.8710
  • a Metabolite formation.

  • b Units are 106 cells/ml.

  • c Units are milligrams of protein per milliliter.

  • d Conditions also applied for inhibition experiments.

  • e Units are picomoles per milliliter.