Table 3. 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 |
| 12α | 313.4±102.9 | 89.49±0.7 | NR |
| 12β | NR | 0 | NR |
| 13α | 455.7±148.6 | 88.50±0.8 | NR |
| 13β | NR | 0 | NR |
| 14α | 303.8±85.9 | 91.39±0.6 | NR |
| 14β | NR | 0 | NR |
| 15α | 477.7±84.9 | 32.89±2.9 | NR |
| 15β | NR | 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.