Table 2 |.
Individual effects of bile acids on bile acid receptors
| Bile acid | FXR EC50 | FXR IC50 | TGR5 EC50 | VDR EC50 | PXR EC50 |
|---|---|---|---|---|---|
| Cholic acid | 100–200 μM197 | NA | 7.72 μM85, >10 μM84, 13.6 μM213 | No effect211 | No effect211 |
| Deoxycholic acid | 50 μM42, 50–75 μM212 | NA | 1.01–1.25 μM85,213 | No effect211 | 50.2 μM211 |
| Chenodeoxycholic acid | 1–2 μM212, 4.5 μM40, 5.2 μM185, 7 μM75, 10 μM41,212, (T, G) 10 μM40, 10–30 μM214, 20 μM41,212, 25–50 μM212, 50 μM42 | NA | 4–4.43 μM84,85, (T) 1.92 μM213, (G) 3.88 μM199 | No effect211 | (T) 104 μM211 |
| Lithocholic acid | 50 μM42 | NA | 35 nM84, (T) 0.33 μM85, 0.53 μM85, 3 μM84 | 8 μM41, 12.1 μM215, 21.6 μM211 | 10.2 μM211 |
| 3-Keto-lithocholic acid | NA | NA | NA | 3 μM75, 6.8 μM215 | 8.3 μM211 |
| Ursodeoxycholic acid | No effect40 | NA | 36.4 μM213, No effect85 | No effect75 | NA |
| α-Muricholic acid | NA | (T) 28 μM191 | NA | 101.7 μM211 | 56 μM211 |
| β-Murichoiic acid | NA | (T) 40 μM202 | NA | No effect211 | No effect211 |
| Hyodeoxycholic acid | NA | NA | 31.6 μM213 | NA | NA |
Note that different studies used different systems (cell lysates and different cell lines) and methods (such as, competitive binding assays, cAMP levels, cAMP-responsive luciferase reporter) to determine EC50 and IC50 values. The individual references should be consulted for details. EC50, the effective concentration for a half maximal response; FXR, farnesoid X receptor; G, values specifically for glycine conjugates; IC50, the concentration that reduces the response by half; NA, not applicable; PXR, pregnane X receptor; T, values specifically for taurine conjugates; TGR5, Takeda G protein-coupled receptor 5; VDR, vitamin D receptor.