An effective antagonist of apelin receptor (Ki = 82 nM; IC50 = 93 nM) that antagonizes the inhibitory affect of [Pyr1]-Apelin-13 on forskolin-induced cAMP accumulation in CHO-K1-APJ cells.
CAT No: R0967
CAS No:1313027-43-8
Synonyms/Alias:MM 54;1313027-43-8;H-Cys(1)-Arg-Pro-Arg-Leu-Cys(1)-Lys-His-Cys(2)-Arg-Pro-Arg-Leu-Cys(2)-OH;AKOS030210973;DA-65546;PD079967;G15979;
MM 54 is a synthetic peptide compound recognized for its role as a selective modulator of the melanocortin-4 receptor (MC4R), a G protein-coupled receptor that plays a pivotal part in regulating energy homeostasis and feeding behavior. As a research tool, MM 54 provides a valuable means for investigating the physiological and biochemical pathways associated with the melanocortin system, particularly in the context of neuroendocrine signaling and metabolic regulation. Its specificity and well-characterized activity profile make it an important asset for studies aimed at deciphering the molecular mechanisms underlying central nervous system function and peptide-receptor interactions.
Receptor pharmacology: MM 54 is frequently used in receptor binding and functional assays to delineate the pharmacological properties of the MC4R. By acting as a selective antagonist or modulator, it enables researchers to dissect receptor-ligand interactions, evaluate receptor specificity, and quantify downstream signaling events. These studies are essential for mapping the structural determinants of MC4R function and for distinguishing the unique contributions of different melanocortin receptor subtypes within complex biological systems.
Neuroendocrine research: In neuroendocrinology, MM 54 serves as a critical probe for exploring the role of MC4R in hypothalamic signaling pathways. Its application in in vitro and ex vivo models allows scientists to examine how melanocortin signaling influences neuropeptide release, synaptic plasticity, and neuronal excitability. Such investigations provide foundational insights into the mechanisms by which central peptides regulate appetite, energy expenditure, and neuroendocrine feedback loops.
Metabolic studies: The compound is employed in metabolic research to investigate the regulatory effects of MC4R on energy balance, glucose metabolism, and adiposity at the cellular and molecular levels. By modulating receptor activity in relevant cell lines or tissue explants, MM 54 enables the assessment of gene expression changes, second messenger cascades, and metabolic enzyme activity. These approaches are instrumental in elucidating the intricate networks that govern metabolic homeostasis and may inform the identification of new molecular targets for metabolic research.
Peptide-receptor interaction analysis: MM 54 is a valuable tool in structure-activity relationship (SAR) studies designed to characterize peptide-receptor binding dynamics. Its defined sequence and activity facilitate the systematic evaluation of amino acid substitutions, conformational constraints, and ligand modifications that affect MC4R affinity and efficacy. Such analyses support the rational design of novel peptide analogs and contribute to a deeper understanding of peptide-based modulation in the melanocortin system.
Peptide synthesis and assay development: In the context of peptide chemistry and assay development, MM 54 is utilized as a reference standard or control compound for the validation of new analytical methods, bioassays, and screening protocols targeting MC4R. Its reproducible activity profile aids in the calibration of assay sensitivity and specificity, ensuring reliable measurement of receptor-mediated responses. This application is vital for the advancement of high-throughput screening platforms and the optimization of experimental protocols in peptide research.
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