Table 2. Comparison of (S)-17a and (S)-11b.
(S)-17a | (S)-11b | |
---|---|---|
Ki (hCRTH2) (nM) | 35 | 15 |
eosinophil chemotaxis IC50 (nM) | 47 | 7.4 |
hWB assay IC50 (nM) | 150 | 69 |
Fu (h, r, m, %) | 2.0/1.9/5.0 | 2.3/3.0/6.3 |
Caco-2 permeation Papp (cm/s) | 0.6 | 0.2 × 10–6 |
clearance in mouse (L/kg/h) | 0.8 | 0.8 |
oral bioavailability in mouse (Fz, %) | 39 | 9 |
AUC po (5 mg/kg) (h ng/mL) | 2400 | 580 |