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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)
  1. a Maximal reference compound (efficacy = 1.0) ; efficacy of other compounds are relative to the maximal reference compound.