Cetrorelix Acetate (SB-75 acetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
CAT No: HB00121
CAS No:130143-01-0
Synonyms/Alias:130143-01-0;Cetrorelix diacetate;Cetrotide acetate;Cetrotide;W9Y8L7GP4C;Cetrorelix (diacetate);SB-075 ACETATE;Cetrorelix acetate [MI];Cetrorelix acetate [JAN];UNII-W9Y8L7GP4C;Cetrorelix acetate [USAN];Cetrorelix acetate [VANDF];Cetrorelix acetate [MART.];Cetrorelix acetate [WHO-DD];D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N5-(aminocarbonyl)-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-, diacetate (salt);Cetrorelix acetate (MART.);D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N(sup 5)-(aminocarbonyl)-D-ornithyl-L-leucyl-L-argyinyl-L-prolyl-, acetate (salt);N-Acetyl-3-(2-naphthyl)-D-alanyl-p-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-L-tyrosyl-N(sup 5)-carbamoyl-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-D-alaninamide acetate (salt);SB 075 acetate;NS 75a;Cetrorelixdiacetate;SB-075 diacetate;N-acetyl-3-(naphthalen-2-yl)-D-alanyl-4-chloro-D-phenylalanyl-3-(pyridin-3-yl)-D-alanyl-L-seryl-L-tyrosyl-N(5)-carbamoyl-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-D-alaninamide acetate;SCHEMBL6149471;D 20761;HY-P0009B;EX-A3856;AKOS037748846;Cetrorelix acetate [USAN:JAN:WHO-DD];BS-15110;CS-0134655;D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N5-(aminocarbonyl)-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-, acetate (salt);D81833;Q27895653;N-Acetyl-3-(2-naphthyl)-D-alanyl-p-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-L-tyrosyl-N5-carbamoyl-D-ornithyl-L-leucyl-L-arginyl-L-prolyl-D-alanin-amide acetate;
Cetrorelix is a synthetic decapeptide that functions as a potent gonadotropin-releasing hormone (GnRH) antagonist, widely utilized in biochemical and reproductive biology research. Structurally engineered to competitively bind to GnRH receptors in the pituitary gland, Cetrorelix blocks the endogenous action of GnRH, thereby suppressing the downstream secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Its high receptor affinity and stability render it a valuable tool for elucidating the mechanisms of hormonal regulation in vertebrate systems. Researchers leverage its precise antagonistic activity to dissect the physiological roles of the hypothalamic-pituitary-gonadal (HPG) axis, making it an indispensable compound in both basic and applied endocrinological studies.
Hormonal Regulation Studies: Cetrorelix is extensively applied in investigations of pituitary hormone modulation, enabling researchers to selectively inhibit GnRH-mediated signaling pathways. By introducing this peptide antagonist in vitro or in vivo, scientists can achieve controlled suppression of LH and FSH release, facilitating the analysis of downstream effects on steroidogenesis, gametogenesis, and reproductive tissue development. Such studies are crucial for advancing the understanding of endocrine feedback loops and the temporal dynamics of hormonal cascades in mammalian systems.
Reproductive Biology Research: The compound is a preferred agent for modeling the physiological consequences of GnRH antagonism in animal models. Its use allows for the experimental manipulation of reproductive cycles, ovulation, and spermatogenesis, providing valuable insights into the regulation of fertility and gonadal function. Researchers often employ Cetrorelix to investigate the impact of acute or chronic suppression of gonadotropins on reproductive tissues, which is instrumental in mapping the molecular underpinnings of reproductive disorders and the development of novel fertility control strategies.
Peptide-Protein Interaction Analysis: As a structurally optimized GnRH antagonist, Cetrorelix serves as a reference molecule in studies probing peptide-receptor interactions. Its defined sequence and well-characterized binding kinetics make it suitable for comparative binding assays, receptor mapping, and structure-activity relationship (SAR) analyses. These applications support the rational design of next-generation peptide therapeutics and the refinement of molecular models describing ligand-receptor specificity within the GnRH receptor family.
Pharmacodynamic and Signal Transduction Research: The peptide's ability to acutely modulate pituitary signaling provides a robust platform for examining the downstream effects of GnRH receptor blockade on intracellular pathways. By employing Cetrorelix in cell-based assays or animal models, researchers can delineate the changes in second messenger systems, gene expression profiles, and protein phosphorylation events associated with gonadotropin suppression. This mechanistic insight is essential for decoding the broader physiological roles of GnRH signaling beyond reproduction, including its involvement in metabolic and neuroendocrine regulation.
Peptide Synthesis and Analytical Method Development: Cetrorelix is frequently utilized as a benchmark compound in the development and validation of peptide synthesis protocols, chromatographic separation techniques, and mass spectrometric assays. Its defined structure and stability under various analytical conditions make it an ideal standard for optimizing purification procedures, calibrating detection methods, and ensuring the reproducibility of peptide-based experimental workflows. These applications are critical for advancing peptide chemistry and ensuring the quality control of research-grade peptide preparations.
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