Table 3.
Kinetic parameters for the metabolism of (S)- and (R)-norKet in pooled HLMs (n=2). A range of (S)- and (R)-norKet concentrations was incubated with HLMs (0.5 mg/ml) at 37°C for 30 min. Substrate concentrations versus velocity were fit using Michaelis-Menten nonlinear regression analyses, where: Vmax, pmol/min/mg protein; Km, μM; and Vmax/Km (in vitro intrinsic clearance, Clint),μL/min/mg protein.
Metabolite | (S)-norKet | (R)-norKet | ||||
---|---|---|---|---|---|---|
Vmax | Km | Vmax/Km | Vmax | Km | Vmax/Km | |
HNK | ||||||
4a | 196.3 | 76.2 | 2.58 | 366.7 | 96.1 | 3.82 |
4c | 837.3 | 75.8 | 11.0 | 825.4 | 54.3 | 15.2 |
4d | 437.5 | 97.0 | 4.5 | 127.2 | 199.8 | 0.64 |
4e | 14.3 | 62.1 | 0.23 | |||
4f | 213.2 | 39.6 | 5.39 | 488.8 | 111.2 | 4.39 |
DHNK | ||||||
DHNK | 437 | 112.6 | 3.88 | 469 | 145.2 | 2.23 |