Relamorelin, a cutting-edge therapeutic peptide, exhibits remarkable potential in the realm of biomedical science. Specifically designed to address the intricate complexities of gastrointestinal system disorders, this prodigious innovation functions as a highly potent and selective agonist for the prestigious ghrelin receptor.
CAT No: R2017
CAS No:661472-41-9
Synonyms/Alias:Relamorelin;Relamorelin [INN];Relamorelin [WHO-DD];Relamorelin [USAN:INN];BIM28131;RM131;UNII-BIW199E18V;661472-41-9;BIM-28131;RM 131;RM-131;BIW199E18V;4-[[(2S)-2-[[(2R)-2-[[(2R)-3-(1-benzothiophen-3-yl)-2-(piperidine-3-carbonylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]piperidine-4-carboxamide;4-Piperidinecarboxamide, 3-benzo(b)thien-3-yl-N-(4-piperidinylcarbonyl)-D-alanyl-D-tryptophyl-L-phenylalanyl-4-amino-;relamorelinum;4-((2S)-2-((2R)-2-((2R)-3-(1-benzothiophen-3-yl)-2-((piperidin-4-yl)formamido)propanamido)-3-(1H-indol-3-yl)propanamido)-3-phenylpropanamido)piperidine-4-carboxamide;4-[(2S)-2-[(2R)-2-[(2R)-3-(1-benzothiophen-3-yl)-2-[(piperidin-4-yl)formamido]propanamido]-3-(1H-indol-3-yl)propanamido]-3-phenylpropanamido]piperidine-4-carboxamide;Relamorelin (USAN/INN);SCHEMBL17513917;DTXCID201517412;GLXC-25336;DA-67147;D10660;
Chemical Name:4-[[(2S)-2-[[(2R)-2-[[(2R)-3-(1-benzothiophen-3-yl)-2-(piperidine-3-carbonylamino)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]piperidine-4-carboxamide
Relamorelin is a synthetic peptide compound that functions as a potent agonist of the ghrelin receptor, also known as the growth hormone secretagogue receptor (GHSR). Structurally derived from the natural gut peptide ghrelin, Relamorelin exhibits enhanced stability and receptor affinity, making it a valuable tool in the study of gastrointestinal motility, appetite regulation, and peptide-receptor interactions. Its unique biochemical profile and targeted mechanism of action have positioned it as an important molecule for advancing peptide pharmacology and gastrointestinal research, as well as for supporting the development of novel modulators of the ghrelin signaling pathway.
Gastrointestinal Motility Research: As a selective GHSR agonist, Relamorelin is widely utilized in experimental models to investigate the physiological and molecular mechanisms underlying gastric emptying and intestinal transit. Researchers employ this peptide to probe the role of ghrelin signaling in regulating smooth muscle contraction, enteric neuronal activity, and the coordination of digestive processes. Its robust and reproducible effects on motility make it an indispensable tool for dissecting the pathways involved in both normal and dysregulated gastrointestinal function.
Peptide-Receptor Interaction Studies: The high specificity and affinity of Relamorelin for the ghrelin receptor enable detailed characterization of ligand-receptor binding dynamics and downstream signaling events. In vitro and ex vivo assays frequently use this compound to elucidate GHSR activation, receptor desensitization, and signal transduction cascades. These studies provide critical insights into the structure-activity relationships of peptide agonists and inform the rational design of next-generation receptor modulators.
Appetite and Energy Homeostasis Investigations: By mimicking the activity of endogenous ghrelin, Relamorelin serves as a powerful experimental probe for exploring the central and peripheral mechanisms that regulate appetite, satiety, and energy balance. Its application in animal models allows researchers to delineate the neuroendocrine circuits influenced by ghrelin signaling, assess the peptide's impact on feeding behavior, and evaluate metabolic outcomes associated with altered receptor activation.
Peptide Drug Development and Optimization: The synthetic nature and optimized pharmacokinetic properties of Relamorelin make it a reference compound in the development of novel peptide-based therapeutics targeting the GHSR pathway. Medicinal chemists and peptide engineers utilize it as a benchmark for assessing the efficacy, stability, and receptor selectivity of new peptide analogs. Comparative studies with Relamorelin facilitate the identification of structural modifications that enhance bioactivity or improve pharmacological profiles, advancing the field of peptide drug discovery.
Analytical and Bioassay Standardization: In laboratory settings, Relamorelin is often employed as a positive control or calibration standard in bioassays designed to quantify ghrelin receptor activity. Its well-characterized pharmacological profile supports assay validation, quality control, and method development for both academic and industrial research applications. The use of such a standardized peptide ensures reproducibility and comparability across experimental platforms, contributing to robust and reliable data generation in peptide pharmacology.
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