Kinetic parameters of E2074 in liver and intestinal microsomes
The figures in parentheses are the standard deviation of estimates.
| Parameter | Rat Liver | Dog Liver | Monkey Liver | Monkey Intestine |
|---|---|---|---|---|
| Km1 (μM) | 7.23 (1.34) | 0.41 (0.34) | 42.44 (7.86) | 34.60 (7.28) |
| Vmax1 (nmol/min/mg protein) | 1.42 (0.13) | 0.07 (0.03) | 3.58 (0.42) | 0.66 (0.11) |
| Km2 (μM) | NA | 21.50 (4.65) | NA | NA |
| Vmax2 (nmol/min/mg protein) | NA | 0.72 (0.03) | NA | NA |
| r | 1.10 (0.03) | NA | 1.04 (0.02) | NA |
E2074, 2-[(2R)-2-fluoro-3-{(3r)-[(3-fluorobenzyl)oxy]-8-azabicyclo[3.2.1]oct-8-yl}propyl]-4,5-dimethyl-2,4-dihydro-3H-1,2,4-triazol-3-one; Km, Michaelis–Menten constant; r, Hill coefficient; NA, not applicable; Vmax, maximum velocity.