Microsomes | KM | Vmax | Vmax/KM | Contents of CYP in Human Liver Microsomes | EstimatedVmax/KM in Human Liver Microsomes |
---|---|---|---|---|---|
μM | pmol/min/pmol CYP | μl/min/pmol CYP | pmol CYP/mg of protein | μl/min/mg of protein | |
CYP2B6 | 30.7 ± 1.21-a | 2.04 ± 0.361-a | 0.067 ± 0.0121-a | 411-b | 2.71-c (14%)1-d |
CYP2C9 | 30.3 ± 5.3 | 1.73 ± 0.28 | 0.057 ± 0.006 | 96 | 5.5 (29%) |
CYP2C19 | 9.0 ± 1.7 | 1.11 ± 0.22 | 0.124 ± 0.016 | 19 | 2.4 (13%) |
CYP2D6 | 2.6 ± 0.3 | 0.79 ± 0.05 | 0.309 ± 0.022 | 22 | 6.8 (35%) |
CYP3A4 | 45.3 ± 8.5 | 0.57 ± 0.06 | 0.013 ± 0.002 | 142 | 1.8 (9%) |
↵1-a The values are expressed as the mean ± S.D. from three different experiments.
↵1-b Provided in data sheets by the manufacturer.
↵1-c Estimated from theVmax/KM values of cDNA-expressed CYP isoforms and their contents in pooled human liver microsomes.
↵1-d Numbers in parentheses represent the estimatedVmax/KM as a percentage of the total Vmax/KM values of five CYP isoforms (CYP2B6, CYP2C9, CYP2C19, CYP2D6, and CYP3A4).