Inhibition of PDE isozyme activities by E6005 and cilomilast
Data given as the mean maximum inhibition rate at 30 µM ± S.E.M. or mean IC50 values (nM) calculated from concentration-inhibition curves from three separate experiments; 95% confidence intervals are shown in parentheses.
| Compound | PDE Subtype | ||||
|---|---|---|---|---|---|
| PDE1 | PDE2 | PDE3 | PDE4 | PDE5 | |
| E6005 | 46.1 ± 6.2% at 30 µM | 51.6 ± 4% at 30 µM | 69.4 ± 5.4% at 30 µM | IC50 = 2.8 nM (1.6–3.9 nM) | 57.4 ± 7.2% at 30 µM |
| Cilomilast | 12.7 ± 6.2% at 30 µM | 26.6 ± 1.9% at 30 µM | 6.4 ± 1.8% at 30 µM | IC50 = 24 nM (6.1–42 nM) | 19.9 ± 1.6% at 30 µM |