Table 2.
Comparison of PL-8177 (A) and PL-8331 (B) Binding and cAMP Functional Activity at Melanocortin Receptors 2–5.a
| EC50 (nM) |
Emax @ 10 uM (%) |
|||||
|---|---|---|---|---|---|---|
| Ave | Std | n | Ave | Std | n | |
| A. PL-8177 | ||||||
| MC2r | 10000 | 0 | 1 | 15 | 0 | 1 |
| MC3r | 10000 | 0 | 1 | 45 | 0 | 1 |
| MC4r | 510 | 0 | 1 | 87 | 0 | 1 |
| MC5r | 9700 | 424 | 2 | 45 | 8 | 2 |
| B. PL-8331 | ||||||
| MC2r | 10000 | 0 | 1 | 18 | 0 | 1 |
| MC3r | 1 | 0 | 1 | 72 | 0 | 1 |
| MC4r | 0.77 | 0 | 1 | 80 | 0 | 1 |
| MC5r | 15 | 1 | 2 | 50 | 9 | 2 |
aTesting conducted and data generated by CEREP, Inc., a subsidiary of Eurofins Panlabs, Inc. EC50, half maximal effect; Emax, maximal effect; MC, melanocortin; r, receptor.