TABLE 1

Kinetic parameters for each enzyme/substrate combination


Substrate

Enzyme Source

Km

Vmax

CLint
μM nmol/min/nmol P450 ml/min/nmol P450
Diclofenac Baculosomes 5.1 ± 0.9 29 ± 2 5.7
Supersomes 2.6 ± 0.3 14.8 ± 0.4 5.7
RECO 16 ± 2 16.8 ± 0.9 1.1
Reconstituted 30 ± 3 27 ± 1 0.9
HLMa 4.0 19.6b 4.9b
(S)-Flurbiprofen Baculosomes 16.2 ± 0.9 34 ± 1 2.1
Supersomes 21.6 ± 0.8 11.7 ± 0.8 0.54
RECO 120 ± 10 16.8 ± 0.5 0.14
Reconstituted 45 ± 2 11.5 ± 0.2 0.25
HLMc 1.9 4.0b 2.1b
Tolbutamide Baculosomes 103 ± 6 10.1 ± 0.2 0.098
Supersomes 194 ± 29 4.0 ± 0.2 0.021
RECO 1462 ± 50 5.6 ± 0.1 0.0038
Reconstituted 220 ± 19 3.9 ± 0.1 0.018
HLMa 147 3.2b 0.021b
(S)-Warfarin Baculosomes 4.6 ± 0.3 2.33 ± 0.03 0.51
Supersomes 13 ± 2 0.38 ± 0.01 0.029
RECO 32 ± 2 0.698 ± 0.009 0.022
Reconstituted 52 ± 9 1.54 ± 0.07 0.030

HLMd
3.7
0.12b
0.032b
  • a Walsky and Obach (2004).

  • b Converted from literature values using an average CYP2C9 microsomal concentration of 85.4 pmol/mg (Wester et al., 2000).

  • c Tracy et al. (1995).

  • d Hemeryck et al. (1999).