A MC4R antagonist (Ki = 0.16 µM); selective for MC4R over MC3R and MC5R (IC50s = 0.32

ML-00253764 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
1706524-94-8
Storage:
-20
UN-No:
Non-Hazardous - /

ML-00253764 is a melanocortin receptor 4 (MC4R) antagonist (Ki = 0.16 µM).{51180} It is selective for MC4R over MC3R and MC5R (IC50s = 0.32, 0.81, and 2.12 µM, respectively).{51181} ML-00253764 (100 µM) decreases cAMP production induced by [NLE4,D-Phe7]-α-melanocyte stimulating hormone ([NDP]-α-MSH; Item No. 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.  

 

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Description

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

Formal name: 2-[2-[2-(5-bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole, monohydrochloride

Synonyms: 

Molecular weight: 413.7

CAS: 1706524-94-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors||Research Area|Neuroscience|Behavioral Neuroscience|Food Intake

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