Table 1.
Assessment of the metabolic/microsomal stability of G28, CHI3L1-IN-1, K284, and G721–0282.a
| Compound | t1/2 [h] (mouse plasma) | t1/2 [h] (human plasma) | t1/2 [h] (mouse microsomes) | t1/2 [h] (human microsomes) | Clint (mouse, mL/min/mg) | Clint (human, mL/min/mg) |
|---|---|---|---|---|---|---|
| G28 | 3.1 ± 0.3 | 3.9 ± 0.4 | 3.6 ± 0.2 | 4.0 ± 0.1 | 12 ± 1.4 | 8.1 ± 0.6 |
| CHI3L1-IN-1 | 0.9 ± 0.1 | 1.2 ± 0.2 | 1.1 ± 0.2 | 1.5 ± 0.4 | 28 ± 3.8 | 32 ± 4.2 |
| K284 | 1.5 ± 0.2 | 1.9 ± 0.3 | 1.7 ± 0.4 | 2.1 ± 0.3 | 18 ± 1.6 | 22 ± 1.3 |
| G721–0282 | 0.7 ± 0.1 | 0.8 ± 0.1 | 0.8 ± 0.2 | 0.9 ± 0.1 | 42 ± 5.3 | 45 ± 2.7 |
a
Values are mean ± SD (n=3).