ML-00253764 hydrochloride is a brain penetrant nonpeptidicmelanocortin receptor4 (MC4R)antagonist with aK_iandIC₅₀of 0.16 μM and 0.103 μM, respectively^[1].

Ki: 0.16 μM
IC50: 0.103 μM (melanocortin receptor 4)^[1]

ML-00253764 displaces NDP-α-MSH binding with a mean IC₅₀of 0.32 μM, 0.81 μM and 2.12 μM for hMC4-R, hMC3-R and hMC5-R, respectively^[1].
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^[1].

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^[1].
ML-00253764 dissolves in polyethylene glycol 200/saline (1:10) in a volume of 10 mL/kg (For reference only)^[1].

413.71

C₁₈H₁₉BrClFN₂O

1706524-94-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.