Des-Acetyl-Cetrorelix lacks the N-terminal acetyl group found in cetrorelix, increasing overall basicity and altering terminal hydrogen bonding. Researchers compare its folding, solubility, and receptor-binding characteristics with the parent compound. The variant helps elucidate the role of N-terminal capping in peptide performance. Applications include SAR analysis, peptide-stability studies, and analog-design refinement.
CAT No: Z10-101-208
CAS No:121081-09-2
Synonyms/Alias:THAT; 3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-L-tyrosyl-D-citrullyl-L-leucyl-L-arginyl-L-prolyl-D-alaninamide; Des-Acetyl Cetrorelix; D-2Nal-D-Phe(4-Cl)-D-3Pal-Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH2;
Des-Acetyl-Cetrorelix is a synthetic decapeptide that functions as a potent antagonist of gonadotropin-releasing hormone (GnRH) receptors. Structurally related to the clinically utilized cetrorelix, this compound is distinguished by the absence of the terminal acetyl group, which can influence its biochemical properties and receptor interactions. Its ability to competitively inhibit endogenous GnRH binding makes it a valuable tool for modulating the hypothalamic-pituitary-gonadal axis in experimental systems. Researchers leverage its well-characterized mechanism of action to dissect peptide-receptor dynamics, investigate signaling pathways, and advance the understanding of reproductive endocrinology at the molecular level.
Peptide hormone receptor studies: As a GnRH antagonist, Des-Acetyl-Cetrorelix is extensively utilized in receptor binding and signaling assays to elucidate the molecular mechanisms underpinning GnRH receptor activation and inhibition. Its defined structure and high specificity enable precise interrogation of ligand-receptor interactions, facilitating structure-activity relationship (SAR) studies and the mapping of critical binding domains. Such investigations are essential for advancing knowledge of peptide hormone signaling and informing the rational design of novel modulators targeting this receptor family.
Endocrine regulation research: The compound serves as a key reagent in studies focused on the regulation of gonadotropin secretion and feedback mechanisms within the hypothalamic-pituitary-gonadal axis. By selectively blocking GnRH-induced luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release in vitro, Des-Acetyl-Cetrorelix allows researchers to dissect the downstream effects of GnRH antagonism on cellular signaling pathways, gene expression profiles, and hormone biosynthesis. This enables a deeper understanding of endocrine control mechanisms in both normal and perturbed physiological contexts.
Peptide drug development: Owing to its structural similarity to established therapeutic antagonists, Des-Acetyl-Cetrorelix is frequently employed as a reference compound or lead molecule in the development and optimization of next-generation GnRH antagonists. Medicinal chemists and peptide engineers use it to evaluate modifications that enhance metabolic stability, receptor selectivity, or bioactivity. Its application in comparative pharmacological assays helps to identify promising candidates for further preclinical research and to refine the design of peptide-based modulators.
Analytical method validation: The availability of this well-characterized peptide supports the development and validation of analytical techniques, such as high-performance liquid chromatography (HPLC), mass spectrometry, and immunoassays, for the detection and quantification of GnRH analogues. Laboratories utilize Des-Acetyl-Cetrorelix as a calibration standard or quality control reagent, ensuring the accuracy and reproducibility of analytical workflows essential for peptide research and pharmaceutical quality assurance.
Peptide synthesis and modification studies: The compound is also used as a model substrate in the field of peptide chemistry to explore synthetic strategies, post-synthetic modifications, and structure-function relationships. Its defined sequence and functional relevance make it suitable for testing new coupling reagents, protecting group strategies, and purification protocols. Such studies contribute to the advancement of synthetic methodologies and the efficient production of high-quality peptide-based research tools.
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