A MC4R antagonist (Ki = 0.16 µM); selective for MC4R over MC3R and MC5R (IC50s = 0.32, 0.81, and 2.12 µM, respectively); decreases cAMP production induced by [NDP]-α-MSH by 20% in MCR4-expressing HEK293 cell membranes, but has no effect on cAMP levels in MC3R- or MC5R-expressing HEK293 cell membranes at 100 µM; prevents the loss of lean body mass and enhances light-phase food consumption in a LLC mouse xenograft model but does not reduce tumor size at 15 mg/kg