Table 1 Effects of compounds on VDRs
From: Functional evolution of the vitamin D and pregnane X receptors
Common name | Significance | Human VDR EC50 ± SD (relative efficacy) | Mouse VDR EC50 ± SD (relative efficacy) | Xenopus VDR EC50 ± SD (relative efficacy) | Zebrafish VDR EC50 ± SD (relative efficacy) | Sea lamprey VDR EC50 ± SD (relative efficacy) | Ciona VDR/PXR EC50 ± SD (relative efficacy) |
|---|---|---|---|---|---|---|---|
1,25-(OH)2-Vitamin D3 | Vitamin D | 1.2 ± 0.2 nM (1.0a) | 0.6 ± 0.1 nM (1.0a) | 33 ± 3.5 nM (1.0a) | 0.7 ± 0.1 nM (1.0a) | 0.8 ± 0.1 nM (1.0a) | No effect |
1α-Hydroxyvitamin D2 | ligands | 13 ± 1.2 nM (0.88) | 0.8 ± 0.1 nM (0.98) | 624 ± 49 nM (0.58) | 26 ± 1.7 nM (0.78) | 41 ± 3.6 nM (0.88) | No effect |
1α-Hydroxyvitamin D3 |  | 4.3 ± 0.5 nM (0.99) | 0.3 ± 0.04 nM (0.96) | 157 ± 10 nM (0.84) | 18 ± 1.4 nM (0.73) | 94 ± 8.0 nM (0.90) | No effect |
25-Hydroxyvitamin D3 |  | 1.5 ± 0.2 M (1.22) | 0.6 ± 0.1 μM (2.62) | 11 ± 0.8 nM (0.67) | 7.3 ± 0.8 μM (0.91) | 19 ± 2.1 μM (0.63) | No effect |
24(R),25-(OH)2-Vitamin D3 |  | 0.3 ± 0.02 μM (0.9) | 0.3 ± 0.02 μM (1.7) | 11 ± 1.7 μM (0.20) | 0.7 ± 0.06 μM (0.6) | 5.6 ± 0.8 μM (0.9) | No effect |
5α-Petromyzonol | Bile salts from | No effect | No effect | No effect | No effect | No effect | No effect |
5α-Petromyzonol 24-sulfate | sea lamprey | No effect | No effect | No effect | No effect | No effect | No effect |
5α-Cyprinol | Major bile salt | No effect | No effect | No effect | No effect | No effect | No effect |
5α-Cyprinol 27-sulfate | for zebrafish and Xenopus species | No effect | No effect | No effect | No effect | No effect | No effect |
Lithocholic acid | Major human | 11 ± 0.7 (0.12) | 7.1 ± 0.9 (0.36) | No effect | No effect | No effect | No effect |
Glycolithocholic acid | secondary | No effect | 16 ± 2.1 (0.28) | No effect | No effect | No effect | No effect |
Taurolithocholic acid | bile acids and | No effect | 26 ± 3.8 (0.23) | No effect | No effect | No effect | No effect |
Lithocholic acid 3-sulfate | metabolities | No effect | No effect | No effect | No effect | No effect | No effect |
3-Ketolithocholic acid |  | 55 ± 8.1 (0.17) | 20 ± 0.3 (0.58) | No effect | No effect | No effect | No effect |
6-Formylindolo- [3,2-b]-carbazole | Miscellaneous | > 10 (~0.12) | > 10 (~0.08) | > 10 (~0.10) | ~5 (< 0.03) | 2.0 ± 0.3 (0.25) | 0.86 ± 0.081 (1.0a) |
2,3,7,8-Tetrachlorodibenzo-p-dioxin |  | No effect | No effect | No effect | No effect | No effect | 0.23 ± 0.04 (1.80) |