Table 1 Potency and efficacy of SA10SC-RLX in head-to-head comparison with relaxin in different cell types with endogenous or recombinant expression of human or rat RXFP1. Relative EC50s (EC50rel) and Emax were determined with SAS procedure via Biost@t-SPEED-LTS v2.4 internal software using the 4-parameter logistic model. The geometric means of the EC50rel values were calculated with confidence intervals (CI) at 95% level. For Emax comparison between relaxin and SA10SC-RLX, normality hypothesis was confirmed for each group and a paired T test was performed. In the absence of normality hypothesis, a Wilcoxon test was performed. For the EC50 comparison, the same method was applied after log transformation of the value (*P < 0.05 vs relaxin).
Cell type/readout | OVCAR5 (n = 6) | EA.hy926_hRXFP1 (n = 5) | HEK_ratRXFP1 (n = 6) | |||
|---|---|---|---|---|---|---|
cAMP | EC50 (nM) [CI95%] | Emax (%) ± SEM | EC50 (nM) [CI 95%] | Emax (%) ± SEM | EC50 (nM) [CI 95%] | Emax (%) ± SEM |
Relaxin | 1.8 [0.9; 3.4] | 96.2 ± 0.8 | 0.06 [0.04; 0.09] | 100.1 ± 0.7 | 1.4 [0.9; 2.1] | 95.6 ± 0.8 |
SA10-SC-RLX | 0.3* [0.2; 0.7] | 84.1 ± 1.1* | 0.8* [0.3; 1.9] | 93.7 ± 1.1 | 0.3* [0.1; 0.7] | 68.5 ± 2.8* |