Liver microsomal stability of four compounds.
| |||||
|---|---|---|---|---|---|
| Cpd. | Axla IC50 (nM) | Human | Rat | ||
| T 1/2 min | Clint mL min−1 kg−1 | T 1/2 min | Clint mL min−1 kg−1 | ||
| m6 | 5 | 155.9 | CLhep = 11.2 | 153.1 | CLhep = 16.2 |
| CLin vivo = 7.2 | CLin vivo = 12.5 | ||||
| m12 | 12 | 36.2 | CLhep = 48.0 | 6.4 | CLhep = 388.9 |
| CLin vivo = 14.5 | CLin vivo = 48.3 | ||||
| m13 | 22 | 74.2 | CLhep = 23.4 | 15.4 | CLhep = 161.8 |
| CLin vivo = 11.0 | CLin vivo = 41.2 | ||||
| m16 | 5 | 60.6 | CLhep = 28.7 | 28.3 | CLhep = 87.7 |
| CLin vivo = 12.0 | CLin vivo = 33.9 | ||||
| TP-0903 | 15 | 2.7 | CLhep = 645.7 | 4.3 | CLhep = 581.9 |
| CLin vivo = 20.1 | CLin vivo = 50.4 | ||||
These data were used from Table 4.