Table 1. TGR5 and FXR activities of triterpenoids. Data are presented as mean±SEM (n=3).
Name | TGR5 |
FXR |
|
---|---|---|---|
EC50/nmol·L−1 | Efficacy | EC50/nmol·L−1 | |
GW4064 | – | – | 48.82±0.4 |
INT-777 | 395.1±125.6 | 100.0±0.7 | NR |
3α | 1914±473.3 | 95.27±0.7 | NR |
3β | 3214±385.6 | 83.15±4.0 | NR |
EC50 and efficacy generated from human TGR5-based cAMP assay or human FXR-based reporter assay. NR=No response at concentrations up to 100 μmol/L.