Medchemexpress LLC ML-00253764 hydrochloride | 1706524-94-8 | 99.3% | 413.71 | 1 MG

Supplier:  Medchemexpress LLC HY110123100MG

ML-00253764 hydrochloride is a brain penetrant, nonpeptidic melanocortin receptor 4 (MC4R) antagonist with Ki and IC50 values of 0.16 μM and 0.103 μM, respectively. It is capable of crossing the blood-brain barrier.

• Target: melanocortin receptor 4 (MC4R) antagonist.
• Brain penetrant: can cross the blood-brain barrier.
• In vitro activity: displaces NDP-α-MSH binding with a mean IC50 of 0.32 μM for hMC4-R, 0.81 μM for hMC3-R, and 2.12 μM for hMC5-R. At 100 μM, it decreases cAMP production induced by [NLE4,D-Phe7]-α-melanocyte stimulating hormone ([NDP]-α-MSH) by 20% in MC4R-expressing HEK293 cell membranes, but shows no effect on cAMP levels in MC3R- or MC5R-expressing membranes.
• In vivo activity: in CT-26 tumor-bearing BALB/c mice, subcutaneous injection (3, 10, or 30 mg/kg; once daily) showed protection against tumor-induced body weight loss.

Catalog No. 50-003-44006