Potency and species selectivity of palosuran (ACT-058362) on U-II induced intracellular Ca2+ mobilization in CHO cells expressing human or rat UT receptor
Urotensin-II-induced Ca2+ mobilization in the recombinant CHO cells was measured by the FLIPR assay system. The potency of U-II (EC50) was determined in the absence of ACT-058362. The inhibitory potency of ACT-058362 (IC50) was determined on Ca2+ mobilization induced by 30 nM U-II.
Ligand | Human UT Receptor | Rat UT Receptor |
|---|---|---|
| Human U-II (EC50, nM) | 23 ± 2 (n = 10) | 6.5 ± 0.45 nM (n = 7) |
| ACT-058362 (IC50, nM) | 17 ± 0.63 (n = 17) | >10,000 (n = 4) |