CYN 154806 (TFA), a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
CAT No: R1320
CYN 154806 TFA is a synthetic peptide antagonist that targets the melanocortin 4 receptor (MC4R), a G protein-coupled receptor involved in the regulation of energy homeostasis, appetite, and neuroendocrine signaling. As a trifluoroacetate salt form, this compound is widely recognized in biochemical research for its potency and selectivity in modulating MC4R-mediated pathways. Its utility in dissecting the physiological and molecular mechanisms of melanocortin signaling makes it a valuable tool for researchers investigating neuropeptide function, metabolic regulation, and receptor pharmacology.
Receptor Antagonism Studies: As a highly selective MC4R antagonist, CYN 154806 TFA is extensively employed in studies aiming to elucidate the functional roles of melanocortin receptors within the central nervous system and peripheral tissues. By competitively inhibiting endogenous agonists at the MC4R, it enables researchers to specifically interrogate receptor-mediated signaling events, facilitating the identification of downstream effectors and regulatory feedback mechanisms. This targeted approach is critical for distinguishing MC4R-dependent processes from those mediated by related melanocortin receptors.
Metabolic Pathway Investigation: The compound is instrumental in probing the complex interplay between neuropeptide signaling and metabolic control. By blocking MC4R activity, investigators can model the effects of receptor inhibition on energy expenditure, feeding behavior, and glucose metabolism in cellular and animal models. These studies contribute to a deeper understanding of the molecular circuits that govern appetite regulation and energy balance, providing mechanistic insights that inform broader research in endocrinology and metabolic disease.
Peptide Structure-Activity Relationship (SAR) Analysis: As a synthetic peptide, CYN 154806 TFA serves as a reference compound in structure-activity relationship studies focused on the melanocortin receptor family. Researchers utilize its well-characterized antagonist profile to benchmark novel analogues and to delineate the structural features critical for receptor binding and functional selectivity. Such SAR investigations are essential for rational peptide design, optimization of pharmacological properties, and the development of new research tools targeting G protein-coupled receptors.
Neuroendocrine Function Research: The ability of CYN 154806 TFA to modulate MC4R signaling has established its value in studies exploring the neuroendocrine regulation of stress, reproduction, and energy homeostasis. By selectively antagonizing MC4R, it allows for the dissection of central and peripheral neuropeptide pathways, supporting investigations into the hormonal and neuronal networks that integrate metabolic and behavioral responses to environmental cues.
In vivo and in vitro Pharmacology: The compound is frequently used in both in vitro and in vivo experimental systems to validate the specificity and efficacy of MC4R-targeted interventions. In cellular assays, it facilitates the characterization of receptor pharmacodynamics, signal transduction cascades, and ligand-receptor interactions. In animal models, its application enables the assessment of physiological outcomes following acute or chronic MC4R blockade, thereby advancing the preclinical understanding of melanocortin system modulation in health and disease research contexts.
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