Table 2

Turnover numbers for Rat P450 enzymes with fluorometric substrates2-a

Rat P450 IsoformSubstrate
AMMCCMCCECMFCBFCDBFBQBzRes
CYP1A12-b 3.43 78 1.030.34 0.211 5.7 1.35
CYP1A22.211.381.320.0412.30.62
CYP2A12-c
CYP2A20.040.080.260.0302.8
CYP2B10.240.452.82 3.70 2.50.82
CYP2C62.842.14 11.5 2.620.0211.90.02
CYP2C111.530.555.570.130.0650.05
CYP2C120.241.5
CYP2C130.210.740.0030.01
CYP2D10.010.090.250.1595.30.02
CYP2D2 5.9 0.080.340.1944.4
CYP2E12-c 0.630.102.11
CYP3A10.010.081.330.0278.40.06
CYP3A20.010.151.040.015 9.8 0.09
Substrate concentration (μM)204040505024050
Incubation time (min)3030303030303030
Enzyme concentration (nM)2-d 5050502-e 5050505050
  • 2-a  Values, expressed as picomole product per minute per picomole enzyme, represent the mean of duplicate determinations. Ranges were on average <10% of the mean. Bold values indicate the highest catalytic activity within the panel.

  • 2-b  Dashes indicate activity was below the limit of detection which was considered as that corresponding to a signal to background ratio of approximately 1.5. These values and their substrates were 0.05 min−1, AMMC; 0.05 min−1, BFC; 0.008 min−1, CMC; 0.008 min−1, CEC; 0.003 min−1, DBF; 0.05 min−1, MFC; 1.0 min−1, BQ; and 0.008 min−1, BzRes.

  • 2-c  Microsomes from human lymphoblastoid cells engineered to express the rat enzyme.

  • 2-d  Concentration for all enzymes was 50 nM except for CYP2A1 (20 nM) and for CYP2E1 (87 nM).

  • 2-e  Concentration for all enzymes was 50 nM except for CYP1A1, which was 2.5 nM.