Table 1. Comparison of (S)-9b and (S)-11b.
(S)-9b | (S)-11b | |
---|---|---|
Ki (hCRTH2) (nM) | 13 | 15 |
eosinophil chemotaxis IC50 (nM) | 62 | 7.4 |
hWB assay IC50 (nM) | 1800 | 69 |
Fu (h, r, m, %) | <1%/ ND/ND | 2.3/3.0/6.3 |
Caco-2 permeation Papp (cm/s) | 1.8 × 10–6 | 0.2 × 10–6 |
clearance in rat (L/kg/h) | 0.72 | 0.15 |
oral bioavailability in rat (Fz, %) | 5 | 6 |