Setmelanotide (RM-493) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.
CAT No: HB00098
CAS No:920014-72-8
Synonyms/Alias:Setmelanotide;920014-72-8;RM-493;BIM-22493;Setmelanotida;Setmelanotide acetate;UNII-N7T15V1FUY;N7T15V1FUY;(4R,7S,10S,13R,16S,19R,22R)-22-[[(2S)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-13-benzyl-10-[3-(diaminomethylideneamino)propyl]-16-(1H-imidazol-5-ylmethyl)-7-(1H-indol-3-ylmethyl)-19-methyl-6,9,12,15,18,21-hexaoxo-1,2-dithia-5,8,11,14,17,20-hexazacyclotricosane-4-carboxamide;1504602-49-6;L-Cysteinamide, N2-acetyl-L-arginyl-L-cysteinyl-D-alanyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-, cyclic (2->8)-disulfide;Setmelanotide [USAN:INN];Setmelanotidum;Setmelanotide [USAN];Setmelanotide (RM-493);SETMELANOTIDE [INN];SETMELANOTIDE [WHO-DD];GTPL9272;CHEMBL3301624;SCHEMBL21840385;DTXSID501032320;EX-A5542;BDBM50581319;AT23144;CS-6399;DB11700;IRC-022493;DA-67236;DA-77812;HY-19870;Q21098917;RM-493; BIM-22493; IRC-022493;N2-acetyl-L-arginyl-L-cysteinyl-D-alanyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-L-cysteinamide, cyclic (2-8)-disulfide;
Setmelanotide is a synthetic peptide that functions as a selective agonist of the melanocortin-4 receptor (MC4R), a critical component in the regulation of energy homeostasis and appetite signaling within the central nervous system. Structurally derived to mimic endogenous melanocortin peptides, it exhibits high affinity and specificity for MC4R, making it an essential tool in biochemical investigations of melanocortin pathways. Its ability to modulate intracellular signaling cascades downstream of MC4R activation has positioned it as a valuable reagent for elucidating the molecular mechanisms governing metabolic regulation and neuroendocrine function.
Peptide receptor pharmacology: In receptor binding and activation studies, Setmelanotide enables detailed analysis of MC4R pharmacodynamics and pharmacokinetics. Researchers utilize this peptide to characterize receptor-ligand interactions, investigate receptor selectivity profiles, and assess downstream G-protein-coupled receptor (GPCR) signaling events. These investigations provide critical insights into the structure-activity relationships that underlie MC4R modulation and inform the design of selective ligands for research purposes.
Signal transduction studies: The compound serves as a reliable tool for dissecting intracellular signaling pathways activated by MC4R engagement. By applying Setmelanotide to in vitro cell culture systems or ex vivo tissue models, investigators can monitor second messenger cascades such as cyclic AMP production, protein kinase A activation, and downstream transcriptional responses. These studies are instrumental in mapping the molecular circuitry of energy balance and neuropeptide signaling.
Metabolic research: Setmelanotide is widely employed in metabolic studies to probe the neurobiological regulation of appetite and body weight. Its selective activation of MC4R allows for controlled manipulation of hypothalamic signaling networks implicated in feeding behavior and energy expenditure. Researchers leverage these properties to investigate the genetic, molecular, and physiological determinants of metabolic disorders, advancing understanding of homeostatic mechanisms in energy regulation.
Peptide screening and assay development: The high specificity and potency of Setmelanotide make it a preferred reference compound in assay development for MC4R activity. It is routinely used as a positive control in high-throughput screening platforms, radioligand binding assays, and functional bioassays designed to identify novel MC4R modulators or to validate assay sensitivity and robustness. This role is critical in both academic and industrial research settings where reliable assay calibration is essential.
Structure-activity relationship (SAR) analysis: The defined molecular structure of Setmelanotide provides a benchmark for comparative studies aimed at optimizing peptide-based MC4R ligands. Researchers employ it as a standard in SAR analyses to evaluate the effects of amino acid substitutions, cyclization, or other chemical modifications on receptor affinity, selectivity, and functional efficacy. These comparative studies support rational design strategies for next-generation research peptides targeting melanocortin receptors.
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