TABLE 6

Melanocortin receptor selectivity of DCPMP

The affinities (IC50 values) of DCPMP for recombinant human MC1R, MC3R, MC4R, and MC5R in HEK293 cells were determined using traditional radioligand displacement assays in the presence of 0.04 nM 125I-NDP-α-MSH for MC1R (Kd, 0.037 nM); 0.035 nM 125I-NDP-α-MSH for MC3R (Kd, 0.24 nM); 0.02 nM 125I-NDP-α-MSH for MC4R (Kd, 0.5 nM); 0.035 nM 125I-NDP-α-MSH for MC5R (Kd, 0.53 nM).

Ligand DCPMPInhibition at 10 μMIC50MC4R Selectivity
%μM
MC4R880.0251
MC1R15>10>400
MC3R703.07123
MC5R684.04162