Table 1 Characteristics of binding of L3 and D3 derivatives to the LBD of LXRα and β.
From: Vitamin D and lumisterol derivatives can act on liver X receptors (LXRs)
Compounds | LXRα | LXRβ | ||
|---|---|---|---|---|
EC50 (M) | IC50 (M) | EC50 (M) | ||
D3 derivative | 20(OH)D3 | 1.5 × 10–8 ± 7.1 × 10–10 (n = 2) | N/A | 2.6 × 10–6 ± 2.7 × 10–6 (n = 2) |
25(OH)D3 | 1.1 × 10–8 ± 1.1 × 10–8 (n = 2) | N/A | 3.8 × 10–6 ± 1.7 × 10–6 (n = 2) | |
20,23(OH)2D3 | 1.1 × 10–6 ± 1.5 × 10–6 (n = 2) | N/A | 2.6 × 10–5 ± 3.4 × 10–5 (n = 2) | |
20,25(OH)2D3 | 3.5 × 10–7 ± 5.5 × 10–7 (n = 3) | N/A | 2.1 × 10–6 | |
1,20,23(OH)3D3 | N/A | 2.1 × 10–6 | 1.6 × 10–6 | |
1,20,25(OH)3D3 | N/A | 2.3 × 10–6 ± 7.1 × 10–8 (n = 2) | 3.8 × 10–9 | |
1,20(OH)2D3 | N/A | 3.5 × 10–6 ± 3.1 × 10–6 (n = 2) | 2.7 × 10–7 ± 2.0 × 10–7 (n = 2) | |
1,25(OH)2D3 | N/A | 1.1 × 10–6 ± 1.3 × 10–6 (n = 2) | 1.4 × 10–5 ± 1.8 × 10–5 (n = 2) | |
D3 | 7.6 × 10–7 ± 1.0 × 10–6 (n = 2) | N/A | 8.9 × 10–7 ± 3.0 × 10–7 (n = 2) | |
L3 derivative | 20(OH)L3 | 1.8 × 10–6 ± 2.5 × 10–6 (n = 2) | N/A | 2.1 × 10–8 ± 2.4 × 10–8 (n = 2) |
22(OH)L3 | 6.4 × 10–7 ± 7.6 × 10–7 (n = 3) | N/A | 1.4 × 10–5 ± 1.7 × 10–5 (n = 2) | |
24(OH)L3 | 3.6 × 10–6 ± 8.5 × 10–7 (n = 2) | N/A | 1.3 × 10–6 ± 7.1 × 10–7 (n = 2) | |
20,22(OH)2L3 | 1.5 × 10–6 ± 1.4 × 10–6 (n = 2) | N/A | 2.0 × 10–6 ± 4.2 × 10–7 (n = 2) | |
25(OH)L3 | 1.4 × 10–7 ± 2.3 × 10–7 (n = 3) | N/A | 1.9 × 10–6 | |
(25R)-27(OH)L3 | 8.2 × 10–7 ± 1.2 × 10–6 (n = 3) | N/A | 5.5 × 10–7 | |
(25S)-27(OH)L3 | 2.6 × 10–8 ± 2.0 × 10–8 (n = 3) | N/A | 1.3 × 10–9 | |
L3 | 2.5 × 10–7 ± 9.9 × 10–8 (n = 2) | N/A | 1.1 × 10–7 | |
pD derivative | 17,20(OH)2pD | 3.0 × 10–5 ± 3.9 × 10–5 (n = 2) | N/A | 2.6 × 10–6 ± 7.1 × 10–7 (n = 2) |
