ML-00253764 HYDROCHLORIDE

ML-00253764 displaces NDP-α-MSH binding with a mean IC ₅₀ of 0.32 μM, 0.81 μM and 2.12 μM for hMC4-R, hMC3-R and hMC5-R, respectively. ML-00253764 (100 µM) decreases cAMP production induced by [NLE4,D-Phe7]-α-melanocyte stimulating hormone ([NDP]-α-MSH) by 20% in MC4R-expressing HEK293 cell membranes, but has no effect on cAMP levels in MC3R- or MC5R-expressing membranes.

ML-00253764 (subcutaneous injection; 3, 10, or 30 mg/kg; once daily) shows protection against tumor-induced body weight loss upon chronic, peripheral dosing in CT-26 tumor bearing BALB/c mice.ML-00253764 dissolves in polyethylene glycol 200/saline (1:10) in a volume of 10 ml/kg.