Table 1. In vitro pharmacology of MK-2305.
| Receptor | EC50 (nM) | % Activation |
|---|---|---|
| Rat GPR40 (FFAR1) | 6 ± 2.9 | 166 ± 311 |
| Rat GPR120 (FFAR4) | >10, 000 | 9 ± 7 @ 10 μM |
| Human GPR41 (FFAR3) | 12711 | 85 @ 25 μM |
| Human GPR43 (FFAR2) | >25, 000 | 61 @ 25 μM |
| Rat PPARα | >10, 000 | -0.2 @ 10 μM |
| Rat PPARδ | >10, 000 | -0.1 @ 10 μM |
| Rat PPARγ | >10, 000 | 3.1 @ 10 μM |
MK-2305 potency and selectivity is examined against the GPR40 receptor, other FFAR family members, and peroxisome proliferator-activated receptors (PPAR). All receptors are rat orthologs, except GPR41 and GPR43 which are human. Values are mean ± SD.
1Relative to AMG837 (% Activation, 173%) and AM1638 (%Activation, Act 373%).