Efficacy of compound 2 following steady-state infusion Shown are data from two experiments in which compound was delivered from minipumps implanted s.c. For the lower plasma concentration, one pump/mouse contained compound at 1 mg/ml; for the higher concentration, two pumps/mouse were used, each containing 7.5 mg/ml. Mice were challenged i.n. with 10 μg of mEotaxin.
Experiment 1 | Experiment 2 | |||||
|---|---|---|---|---|---|---|
| % Reduction in BAL Eosinophils | 67 | 96 | 50 | 85 | ||
| Steady-state plasma concentration (nM) | 24 ± 1.2 | 216 ± 20 | 57 ± 12 | 208 ± 42 | ||
| Freea plasma concentration (nM) | 1.2 ± 0.06 | 10.8 ± 1 | 2.9 ± 0.6 | 10.4 ± 2.1 | ||
| Multiple of chemotaxis IC50 (0.2 nM) | 6 | 54 | 14 | 52 | ||
| Multiple of binding IC50 (3 nM) | 0.4 | 3.6 | 1 | 3.5 | ||
↵* Calculated based on mouse protein binding = 95%