Table 2

Effect of DEM concentration on hepatocyte concentrations and fractions unbound in media, cells and microsomes

Initial ConcentrationCell Concentration2-aCell-to-Media Partition CoefficientFraction Unbound
Media2-bCells2-cMicrosomes
μM μM
0.518.3  ± 2.448.3  ± 7.20.85  ± 0.020.021  ± 0.0031.00  ± 0.02
5208  ± 1753.3  ± 3.40.83  ± 0.010.019  ± 0.0021.02  ± 0.02
501373  ± 8533.5  ± 1.50.89  ± 0.010.030  ± 0.0010.96  ± 0.06
5007154  ± 121915.9  ± 3.10.94  ± 0.010.064  ± 0.0110.96  ± 0.01
  • 2-a Calculated from eq. 2.

  • 2-b Calculated from eq. 5.

  • 2-c Calculated from eq. 3.