Table 2. 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 | 469.0±94.3 | 100.0±0.7 | NR |
8α | 577.4±86.3 | 89.77±1.2 | NR |
8β | 7082±453.6 | 87.67±1.3 | NR |
9α | 3190±443.8 | 90.19±1.3 | NR |
9β | 3979±994.1 | 93.04±0.8 | NR |
11α | 237.8±73.6 | 91.63±0.4 | NR |
11β | 1867±432.9 | 84.03±1.5 | 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.