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Potency of RDX8940 compared with other TGR5 agonists
| Cellular TGR5 cAMP EC50 |
||
|---|---|---|
| Agonist | EC50, nM | Efficacy, % |
| Mouse | ||
| INT-777 | 2,500 | 92 |
| GPBAR-A | 50 | 100 |
| RDX8940 | 0.25 | 100 |
| Human | ||
| INT-777 | 10,000 | 104 |
| GPBAR-A | 130 | 101 |
| RDX8940 | 2.5 | 92 |
EC50, concentration that produces 50% of the maximum effect; TGR5, G protein-coupled bile acid receptor.
