Mean EC50 values and Emax values for different IP receptor agonists in cAMP accumulation assays determined in human PASMC or T-REx-HEK-high hIP and T-REx-HEK-low hIP cells
| PASMC–cAMPa | HEK–high hIPb | HEK–low hIPb | ||||
|---|---|---|---|---|---|---|
| EC50 (σg) | Emax (S.D.) | EC50 | Emax | EC50 | Emax | |
| ACT-333679 | 214 nM (1.1) | 56% (5%) | 29 nM (26 nM, 33 nM) | 97% (95%, 98%) | 277 nM (270 nM, 285 nM) | 45% (51%, 39%) |
| Selexipag | ND | 29% (6%) | 813 nM (790 nM, 837 nM) | 85% (85%, 84%) | ND | ND |
| Beraprost | 94 nM (1.1) | 104% (7%) | 8.6 nM (8.4 nM, 8.9 nM) | 89% (91%, 86%) | 135 nM (119 nM, 153 nM) | 93% (90%, 96%) |
| Iloprost | 16 nM (1.1) | 100% (0%) | 0.53 nM (0.42 nM, 0.67 nM) | 100% (100%, 100%) | 10 nM (7.8 nM, 13 nM) | 100% (100%, 100%) |
| Treprostinil | 107 nM (1.1) | 107% (4%) | 11 nM (11 nM, 12 nM) | 96% (97%, 95%) | 264 nM (200 nM, 348 nM) | 108% (110%, 106%) |
Emax, maximal efficacy compared with that of iloprost; σg, geometric standard deviation; ND, not determined; S.D., arithmetic standard deviation.
↵a For PASMC, EC50 values were derived using the individual curve-intrinsic maxima, and their geomean is shown. For Emax, arithmetic mean is shown; n = 3 measurements.
↵b For HEK cells, EC50 values were derived using the individual curve–intrinsic maxima. Shown is the geometric mean with individual values in brackets. Emax: Shown are the arithmetic means, with individual values in brackets (n = 2 measurements).