Influence of 5-fold changes in protein and enzyme concentration on the estimated values of fumic, v, CLint, t1/2, and apparent Km
| Condition 1 | Condition 2 | -Fold Change | ||
|---|---|---|---|---|
| Compound A | ||||
| Protein (mg/ml) | 0.46 | 2.3 | ↑2-a | 5 |
| CYP450 (μM) | 0.2 | 1 | ↑ | 5 |
| fumic | 0.055 ± 0.005 | 0.012 ± .002 | ↓ | 5 |
| t 1/2 (min) | 18 ± 1 | 17 ± 2 | ↔ | 1 |
| v (pmol/ml/min) | 85 ± 4 | 18 ± 2 | ↓ | 5 |
| CLint,app(ml/min/kg) | 80 ± 4 | 17 ± 2 | ↓ | 5 |
| V max (pmol/min/mg) | 1200 ± 100 | 1100 ± 200 | ↔ | 1 |
| K m,app (μM) | 13 ± 2 | 70 ± 20 | ↑ | 5 |
| CLint(ml/min/kg)2-b | 1500 | 1400 | ↔ | 1 |
| K m(μM)2-b | 0.72 | 0.84 | ↔ | 1 |
| Compound B | ||||
| Protein (mg/ml) | 0.46 | 2.3 | ↑ | 5 |
| CYP (μM) | 0.20 | 1 | ↑ | 5 |
| fumic | 0.86 ± 0.01 | 0.69 ± 0.03 | ↔ | 1 |
| t 1/2 (min) | 19 ± 0 | 5.9 ± 0.2 | ↓ | 3 |
| v (pmol/ml/min) | 79 ± 1 | 50 ± 2 | ↓ | <2 |
| CLint,app(ml/min/kg) | 76 ± 1 | 48 ± 2 | ↓ | <2 |
| V max (pmol/min/mg) | 330 ± 10 | 280 ± 10 | ↔ | 1 |
| K m,app (μM) | 2.9 ± 0.3 | 4.9 ± 0.3 | ↑ | <2 |
| CLint(ml/min/kg)2-b | 88 | 70 | ↔ | 1 |
| K m(μM)2-b | 2.5 | 3.4 | ↔ | 1 |