IC50 values for various RPL545 and RPL565 against TNFα production by human monocytes stimulated with LPS and proliferation of human mononuclear cells with PHA Values are expressed as geometric mean together with 95% confidence interval of n subjects.
Compound | IC50 | n |
|---|---|---|
| TNFα production | ||
| RPL554 | 0.52 μM (0.38–0.69) | 5 |
| RPL565 | 0.25 μM (0.18–0.35) | 6 |
| Siguazodana | >100 μM | 3 |
| CDP840b | 92 nM (50–167) | 6 |
| Proliferation | ||
| RPL554 | 0.46 μM (0.239–0.897) | 6 |
| RPL565 | 2.90 μM (1.56–5.41) | 6 |
↵ a Ki values for siguazodan against PDE3 (3 μM) and PDE4 (>100 μM) (Nicholson and Shahid, 1994)
↵ b Ki values for CDP840 against PDE3 (>100 μM) and PDE4 (12 nM) (Hughes et al., 1996)