Table 1.
Densitometric determination of EC50s (μM) and 95% CI of diguanides on ACC and AMPK phosphorylation and IC50s on S6 phosphorylation.
| A | DG4 | DG5 | DG6 | DG7 | DG8 | DG10 | DG8N |
|---|---|---|---|---|---|---|---|
| pACC | >500 n = 3 | 11.0 (5.2–23.3) n = 3 | 2.4 (1.3–4.6) n = 4 | 3.4 (1.8–6.2) n = 5 | 3.1 (1.3–7.6) n = 3 | 2.2 (1.0–4.9) n = 4 | >500 n = 3 |
| pAMPK | >500 n = 2 | 12.9 (4.7–35.1) n = 3 | 1.4 (0.6–3.0) n = 3 | 3.7 (1.6–8.4) n = 4 | 2.5 (1.5–4.2) n = 3 | 1.2 (0.8–1.8) n = 4 | >500 n = 3 |
| pS6 | >500 n = 3 | 536 (163–1750) n = 3 | 2.8 (1.8–4.1) n = 3 | 4.9 (2.3–10.3) n = 5 | 14.8 (11–19) n = 3 | 3.9 (2.0–7.3) n = 4 | >500 n = 3 |
| B | 2-methyl DG6 | 1-ethyl | 2,2-dimethyl |
|---|---|---|---|
| DG5 | DG5 | ||
| pACC | 16 (7.4–33) n = 3 | >200 n = 3 | >200 n = 3 |
| pAMPK | 27 (18–40) n = 3 | >200 n = 3 | >200 n = 3 |
| pS6 | 32 (24–43) n = 3 | >200 n = 3 | >200 n = 3 |