Table 1.
FLIPRTETRA® Ca2+ Release |
DiscoveRx β-Arrestin |
DiscoveRx Express β-Arrestin |
|
---|---|---|---|
EC50 (nM)a | |||
Oxytocin | 0.30 ± 0.09 | 23 ± 22 | 44.7 |
TC-OT-39 | 5 ± 1 | 310 ± 260 | 480 |
Carbetocin | 3 ± 1 | 5 ± 2 | 5.3 |
Vasopressin | 5 ± 2 | 1600 ± 900 | 2680 |
Efficacy (% OXT Response)b | |||
TC-OT-39 | 102 | 51 ± 6 | 48 |
Carbetocin | 92 | 32 ± 5 | 32 |
Vasopressin | 105 | 41 ± 6 | 38 |
Potencies and efficacies of the DiscoveRx Express cell lines were run as single points only.
Efficacies were calculated considering the oxytocin response as 100%. The DiscoveRx Express refers to the PathHunter™ eXpress β-Arrestin GPCR Kits using the assay-ready, frozen PathHunter™ eXpress cells available through the manufacturer.