Potency values (EC50 and IC50) of agonists in CHO-FFA4, CHO-FFA1 and HT29 cells.
| Class | Compound | CHO-FFA4 cell | CHO-FFA1 cell | HT 29 cell | |||
|---|---|---|---|---|---|---|---|
| EC50 (μM) | Desensitizationa IC50 (μM) | EC50 (μM) | Desensitizationb IC50 (μM) | EC50 (μM) | Desensitizationc IC50 (μM) | ||
| Class 1, endogenous ligand | ALA | 12.54 ± 0.95 | 24.58 ± 3.55 | 28.66 ± 0.94 | 67.60 ± 23.48 | 50.88 ± 10.01 | ∼153 |
| Class 2, FFA4 selective ligand | TUG891 | 0.16 ± 0.01 | 0.12 ± 0.01 | ∼32 | 4.98 ± 1.29 | 0.29 ± 0.03 | 0.48 ± 0.12 |
| GSK137647A | 0.34 ± 0.07 | 0.67 ± 0.12 | / | / | 2.98 ± 0.64 | 18.38 ± 6.54 | |
| Class 3, FFA1 selective ligand | TAK875 | / | / | 0.031 ± 0.0045 | 0.0016 ± 0.00041 | / | / |
| Class 4, non-selective ligand | GW9508 | 3.62 ± 0.50 | 5.04 ± 0.65 | 0.40 ± 0.03 | 0.14 ± 0.01 | 5.33 ± 1.42 | 12.02 ± 2.12 |
a
IC50 to desensitize the DMR of 0.5 μM TUG891 in CHO-FFA4 cells.
b
IC50 to desensitize the DMR of 1 μM GW9508 in CHO-FFA1 cells.
c
IC50 to desensitize the DMR of 5 μM TUG891 in HT29 cells. Slash (/) indicates that the EC50 is greater than the highest concentration tested of 100 μM (GSK137647A) or 20 μM (TAK875). All data represent mean ± s.d. from three independent measurements, each in duplicate (n = 6).