Compound | PDE4 Inhibition IC50 | IL-2a EC50e | IL-5b EC50e | IL-5c EC50e | IL-4c ECe | TNFαd EC50e |
---|---|---|---|---|---|---|
nM | ||||||
AWD 12-281 | 9.71 (0.51) [4] | 50.0 (10.84) [4] | 46.3 (7.25) [3] | 77.0 (10.68) [4] | 121.5 (55.04) [3] | 87.9 (26.60) [3] |
Rolipram | 75.50 (4.56) [4] | 207.0 (43.62) [4] | 338.6 (32.49) [2] | N.D. | N.D. | 322.4 (87.50) [4] |
Cilomilast | 17.80 (2.32) [4] | 160.0 (33.03) [4] | 165.3 (54.53) [2] | N.D. | N.D. | 699.7 (179.64) [3] |
RPR-73401 | 0.41 (0.0075) [4] | N.D. | 2.0 (0.19) [3] | N.D. | N.D. | 4.97 (0.78) [4] |
RS-25344-000 | 0.28f | N.D. | 0.3 (0.37) [4] | N.D. | N.D. | 5.4 (0.75) [4] |
Roflumilast | 0.27 (0.02) [8] | 4.7 (0.88) [4] | 3.4 (1.22) [4] | 6.7 (0.36) [4] | 11.2 (0.78) [4] | 21.2 (1.94) [3] |
Dexamethasone |
| 7.5 (0.51) [3] | 2.9 (0.79) [4] | 88 ± 1.6% inhibition at 10 nM [4] | 59 ± 4.2% inhibition at 10 nM [4] | 6.4 (1.42) [4] |