Table 4. In Vitro and in Vivo Potencies of 39, 41, and Nicotinic Acid.
| 39 | 41 | nicotinic acid | |
|---|---|---|---|
| hu-GPR109a EC50 (nM)a | 59 ± 56 | 49 ± 11 | 100 ± 15 |
| rat-GPR109a EC50 (nM)a | 3 ± 1 | 6 ± 2 | 39 ± 10 |
| m-GPR109a EC50 (nM)a | 4 ± 3 | 15 ± 5 | 29 ± 5 |
| dog-GPR109a EC50 (nM)a | 21 ± 4 | 126 ± 58 | 30 ± 14 |
| cyno-GPR109a (nM)a | 2 ± 1 | ndb | 26 ± 33 |
| hu-GPR109b EC50 (nM)a | 300 ± 105 | 1120 ± 325 | >10000 |
| rat FFA reduction (1 h post 1 mg/kg dosing) | −77% | −14% | −80%c |
| rat TG reduction (1 h post 1 mg/kg dosing) | −49% | −23% | −60%c |
| dog FFA reduction (1 h post 3 mg/kg dosing) | −70% | ndb | −38% |
Data represent an average of multiple determinations (n ≥ 3) ± standard deviation.
nd = not determined.
10 mg/kg dosing.