Table 2. Peptide Agonist Pharmacology at the Mouse MCRsa.
| EC50 (nM) | ||||||
|---|---|---|---|---|---|---|
| peptide | compound ID | sequence | mMC1R | mMC3R | mMC4R | mMC5R |
| NDP-MSH | Ac-Ser-Tyr-Ser-Nle-Glu-His-DPhe-Arg-Trp-Gly-Lys-Pro-Val-NH2 | 0.009 ± 0.002 | 0.08 ± 0.01 | 0.39 ± 0.07 | 0.17 ± 0.02 | |
| Ac-His-DPhe-Arg-Trp-NH2 | Ac-His-DPhe-Arg-Trp-NH2 | 4.2 ± 0.8 | 27 ± 7 | 3.9 ± 0.7 | 1.9 ± 0.2 | |
| LY2112688 | Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH2 | 0.6 ± 0.2 | 0.16 ± 0.05 | 0.048 ± 0.009 | 0.05 ± 0.01 | |
| Setmelanotide | Ac-Arg-c[Cys-DAla-His-DPhe-Arg-Trp-Cys]-NH2 | 0.5 ± 0.2 | 0.08 ± 0.03 | 0.036 ± 0.004 | 0.08 ± 0.02 | |
| 1 | MDE6-5-2c | c[Pro-His-DPhe-Arg-Trp-Dap-Ala-DPro] | 0.24 ± 0.09 | 8 ± 2 | 0.5 ± 0.1 | 0.183 ± 0.009 |
| 2 | MDE8-123cB | c[Pro-His-DPhe-Arg-Trp-Dap-Lys-DPro] | 0.4 ± 0.1 | 7 ± 2 | 0.34 ± 0.08 | 0.21 ± 0.07 |
| 3 | MDE9-30c | c[Pro-His-DPhe-Arg-Trp-Dap-Lys(Ac-Arg)-DPro] | 0.2 ± 0.1 | 5.3 ± 0.2 | 0.31 ± 0.06 | 0.18 ± 0.02 |
| 4 | COR5-117c | c[Pro-His-DPhe-Arg-Trp-Dap-Lys(Ac-Arg-Arg)-DPro] | 0.16 ± 0.04 | 5 ± 1 | 0.26 ± 0.06 | 0.19 ± 0.01 |
| 5 | JLB2-110c | c[Pro-His-DPhe-Arg-Trp-Dap-Lys(Ac-Arg-Arg-Arg)-DPro] | 0.27 ± 0.05 | 8 ± 2 | 0.34 ± 0.09 | 0.29 ± 0.02 |
| 6 | MDE5-149-2c | c[Pro-His-DPhe-Arg-Trp-Asn-Ala-Phe-DPro] | 0.13 ± 0.04 | 22 ± 6 | 1.0 ± 0.2 | 0.32 ± 0.02 |
| 7 | MDE8-128c | c[Pro-His-DPhe-Arg-Trp-Asn-Lys-Phe-DPro] | 0.07 ± 0.01 | 11 ± 4 | 0.29 ± 0.05 | 0.17 ± 0.03 |
| 8 | MDE9-39cB | c[Pro-His-DPhe-Arg-Trp-Asn-Lys(Ac-Arg)-Phe-DPro] | 0.03 ± 0.01 | 4.0 ± 0.4 | 0.27 ± 0.07 | 0.25 ± 0.03 |
| 9 | COR2-138c | c[Pro-His-DPhe-Arg-Trp-Asn-Lys(Ac-Arg-Arg)-Phe-DPro] | 0.026 ± 0.004 | 2.1 ± 0.3 | 0.13 ± 0.03 | 0.28 ± 0.02 |
| 10 | COR2-78c | c[Pro-His-DPhe-Arg-Trp-Asn-Lys(Ac-Arg-Arg-Arg)-Phe-DPro] | 0.04 ± 0.01 | 2.3 ± 0.7 | 0.20 ± 0.05 | 0.37 ± 0.04 |
a
The indicated errors represent the standard error of the mean from at least three independent experiments performed in duplicate.