ML-00253764 (hydrochloride)

ML-00253764 is a melanocortin receptor 4 (MC4R) antagonist (Ki = 0.16 µM). It is selective for MC4R over MC3R and MC5R (IC50s = 0.32, 0.81, and 2.12 µM, respectively). ML-00253764 (100 µM) decreases cAMP production induced by [NLE4,D-Phe7]-alpha-melanocyte stimulating hormone ([NDP]-alpha-MSH, Cay-24475) by 20% in MC4R-expressing HEK293 cell membranes, but has no effect on cAMP levels in MC3R- or MC5R-expressing membranes. It prevents the loss of lean body mass and enhances light-phase food consumption in a Lewis lung carcinoma (LLC) mouse model but does not reduce tumor size when administered at a dose of 15 mg/kg.Formal Name: 2-[2-[2-(5-bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole, monohydrochloride. CAS Number: 1706524-94-8. Molecular Formula: C18H18BrFN2O . HCl. Formula Weight: 413.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30mg/mL, DMF:PBS (pH 7.2) (1:20): 0.5mg/mL, DMSO: 25mg/mL, Ethanol: 1mg/mL. lambdamax: 227, 280 nm. SMILES: BrC1=CC=C(OC)C(CCC2=C(F)C=CC=C2C3=NCCN3)=C1.Cl. InChi Code: InChI=1S/C18H18BrFN2O.ClH/c1-23-17-8-6-13(19)11-12(17)5-7-14-15(3-2-4-16(14)20)18-21-9-10-22-18,/h2-4,6,8,11H,5,7,9-10H2,1H3,(H,21,22),1H. InChi Key: KZUMGPQDDCBFBF-UHFFFAOYSA-N.