TABLE 1

Km and Vmax values for the P450-catalyzed reactions with human liver microsomes and Supersomes and calculated RAFs


P450 Isoform-Substrate (Reported Km Values)

Human Liver Microsomes

Supersomes

RAFa
Km
Vmax b
Km
Vmax b
μM μM
CYP1A2-Phenacetin (30 μM) 20.0 1.79 15.8 2.25 0.63
CYP2C9-Tolbutamide (400 μM) 317 0.10 113 0.04 0.75
CYP2C19-S-Mephenytoin (60 μM) 32.4 0.05 33.5 0.13 0.41
CYP2D6-Dextromethorphan (5 μM) 6.56 2.02 2.50 3.82 0.20
CYP3A4-Testosterone (47 μM)
46.6
1.64
28.5
1.74
0.58
  • a RAF = (Vmax/Km of CYPn in HLM/Vmax/Km of cDNA-expressed CYPn)

  • b Vmax values are represented as peak area ratio of amount of metabolite formed/internal standard.