Estimates of apparent Vmax and Km of HL for CYP probe drugs
CYP | Substrate | Concentration | Microsomal Preparations | Km | Vmax |
---|---|---|---|---|---|
μM | μM | nmol/min/mg | |||
CYP1A2 | phenacetin | 25–150 | MHL-G1-b | 48.7 ± 11.01-a | 2.2 ± 0.3 |
HL-7 | 67.1 ± 15.0 | 0.4 ± 0.2 | |||
HL-14 | 52.1 ± 25.4 | 2.5 ± 1.3 | |||
CYP2C9 | tolbutamide | 25–200 | HL-29 | 152.1 ± 31.5 | 0.03 ± 0.01 |
MHL-B1-c | 163.5 ± 26.7 | 0.26 ± 0.04 | |||
CYP2C19 | omeprazole | 25–150 | HL-29 | 42.2 ± 12.9 | 0.13 ± 0.04 |
MHL-B1-c | 55.1 ± 9.2 | 0.11 ± 0.01 | |||
CYP2D6 | dextromethorphan | 10–75 | MHL-D1-d | 26.2 ± 7.5 | 0.06 ± 0.01 |
HL-29 | 26.9 ± 5.5 | 0.34 ± 0.03 | |||
HL-10 | 22.3 ± 4.0 | 0.20 ± 0.02 | |||
CYP3A | dextromethorphan | 100–750 | HL-10 | 236.3 ± 54.9 | 0.34 ± 0.08 |
MHL-B1-c | 320.8 ± 75.4 | 0.84 ± 0.14 |