An analog of kisspeptin 10, and an antagonist of kisspeptin receptor (KISS1, GPR54) that inhibits kisspeptin-10 stimulation of inositol phosphate (IP) (IC50 = 7 nM) and release of gonadotrophin-releasing hormone (GnRH).
CAT No: R0938
CAS No:1145998-81-7
Synonyms/Alias:Kisspeptin 234;1145998-81-7;ANWNGFGWRF;peptide 234;EX-A7717F;HY-P1196;AKOS024457846;P234;PD079684;CS-0028952;S-1145998-81-7;(2S)-N-({[(1S)-1-[({[(1R)-1-{[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}butyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}methyl)carbamoyl]-2-phenylethyl]carbamoyl}methyl)-2-[(2S)-2-[(2S)-3-carbamoyl-2-[(2R)-2-acetamidopropanamido]propanamido]-3-(1H-indol-3-yl)propanamido]succinamide;
Kisspeptin 234 is a synthetic peptide fragment derived from the kisspeptin family, which plays a pivotal role in the regulation of the hypothalamic-pituitary-gonadal (HPG) axis. As a well-characterized kisspeptin antagonist, it is widely recognized for its ability to modulate the activity of the G protein-coupled receptor GPR54 (also known as KISS1R). The unique inhibitory properties of Kisspeptin 234 have positioned it as a valuable tool for elucidating the physiological and molecular mechanisms underlying reproductive endocrinology, neuroendocrine signaling, and peptide receptor interactions. Its functional specificity and robust bioactivity make it highly relevant for advanced research in peptide signaling pathways and receptor pharmacology.
Reproductive neuroendocrinology research: Kisspeptin 234 is extensively utilized to investigate the regulation of gonadotropin-releasing hormone (GnRH) secretion within the central nervous system. By acting as a competitive antagonist at the KISS1R receptor, it enables researchers to selectively inhibit endogenous kisspeptin signaling, thereby dissecting the contribution of this pathway to the control of puberty onset, fertility, and overall reproductive axis function. The use of this peptide fragment in in vitro and in vivo models provides a precise means to study the feedback mechanisms governing luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release, offering critical insights into the neuroendocrine integration of reproductive processes.
Peptide receptor pharmacology: The antagonist properties of Kisspeptin 234 make it a key reagent for characterizing the pharmacodynamics of the KISS1R receptor. By applying it in receptor binding assays or functional signal transduction studies, researchers can delineate the specificity, affinity, and downstream signaling consequences of kisspeptin-receptor interactions. This approach is instrumental in screening for novel ligands, mapping receptor domains responsible for ligand selectivity, and evaluating the structural determinants of receptor activation versus inhibition. Such studies advance the broader understanding of G protein-coupled receptor modulation in peptide-mediated signaling networks.
Endocrine feedback loop analysis: In studies aiming to unravel the complexity of hormonal feedback circuits, Kisspeptin 234 serves as a strategic tool for selectively blocking kisspeptin-driven pathways. Its application enables the assessment of compensatory mechanisms within the HPG axis and the identification of alternative neuropeptide regulators. By temporarily suppressing kisspeptin activity, investigators can monitor dynamic changes in hormone secretion profiles, gene expression patterns, and neuronal activity, thereby refining models of endocrine homeostasis and adaptive regulation in health and disease states.
Neurobiological pathway mapping: The use of Kisspeptin 234 extends to the mapping of neural circuits involved in reproductive and metabolic control. Through localized administration or targeted delivery in animal models, researchers can identify specific brain regions and neuronal populations responsive to kisspeptin antagonism. Such studies contribute to the delineation of synaptic connectivity, neurotransmitter co-localization, and the integration of external environmental cues with internal hormonal signals. This application is particularly valuable for advancing the neuroanatomical understanding of central reproductive regulation.
Peptide signaling pathway elucidation: As an established kisspeptin pathway inhibitor, Kisspeptin 234 is instrumental in dissecting the broader roles of kisspeptin signaling beyond reproduction, including its involvement in metabolic regulation, stress response, and behavioral modulation. By selectively inhibiting pathway activation, researchers can distinguish direct from indirect effects mediated by kisspeptin, clarify cross-talk with other neuropeptide systems, and explore the evolutionary conservation of peptide signaling mechanisms. Its use in these contexts supports the development of more nuanced models of peptide hormone action and intercellular communication.
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