Functional activity of (E)- and (Z)-guggulsterone in cotransfection assays
| Receptor | IC50 | EC50 (% Eff) | ||
|---|---|---|---|---|
| (E)-GS | (Z)-GS | (E)-GS | (Z)-GS | |
| nM | nM | |||
| GR | 6060 ± 310 | 1740 ± 150 | N.A. | N.A. |
| MR | 1880 ± 390 | 1000 ± 310 | N.A. | N.A. |
| AR | 660 ± 240 | 220 ± 70 | N.A. | N.A. |
| PR | N.A. | N.A. | 740 ± 220 (63) | 1200 (64) |
| ERα | N.A. | N.A. | >5000 (41) | >5000 (59) |
| ERβ | N.A. | N.A. | >5000 (6) | >5000 (15) |
| FXR | >50,000 | >50,000 | N.A. | N.A. |
Eff, efficacy; N.A., not applicable.