Cetrorelix Acetate is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 1.21 nM). It can suppress production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland which inhibits ovulation, exhibit antiproliferative effects and display efficacy against hormone-sensitive cancers in vivo. It is often used to treat hormone-sensitive cancers of the prostate and breast.
CAT No: R0997
CAS No:145672-81-7
Synonyms/Alias: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-D-alaninamide Acetate; 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-D-alaninamide Acetate; SB 075 Acetate
Cetrorelix Acetate is a synthetic decapeptide belonging to the class of gonadotropin-releasing hormone (GnRH) antagonists, renowned for its capacity to modulate reproductive hormone signaling at the hypothalamic-pituitary-gonadal axis. As a peptide compound engineered to bind competitively to GnRH receptors, it effectively inhibits the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Its high specificity, robust receptor affinity, and well-characterized structure make it a valuable tool in the investigation of neuroendocrine regulation and reproductive biology. The compound's stability and well-documented biochemical profile have established it as a standard reagent in both in vitro and in vivo research settings focused on hormonal modulation and peptide-receptor interactions.
Reproductive endocrinology research: Cetrorelix Acetate is widely utilized in studies seeking to elucidate the mechanisms underlying pituitary gonadotropin release. By providing a reliable means to suppress endogenous LH and FSH secretion, it enables controlled investigation of downstream hormonal pathways and feedback mechanisms. Researchers leverage its antagonistic properties to dissect the regulation of gonadal steroidogenesis and to model conditions of altered reproductive hormone dynamics, facilitating detailed analysis of physiological and pathophysiological states in animal models and cell-based systems.
Peptide-receptor interaction studies: The compound serves as a model ligand for studying GnRH receptor pharmacology and signal transduction. Its defined sequence and receptor-binding characteristics make it ideal for affinity assays, receptor mapping, and structure-activity relationship (SAR) analyses. Investigators employ Cetrorelix Acetate in competitive binding experiments to characterize receptor subtypes, probe ligand specificity, and explore the molecular determinants governing antagonist efficacy, advancing the broader understanding of peptide-GPCR interactions.
Assay development and validation: In biochemical and pharmacological assay development, Cetrorelix Acetate is frequently adopted as a standard antagonist control. Its reproducible inhibitory effects on GnRH-mediated signaling provide a robust benchmark for evaluating new GnRH analogs, screening for novel modulators, and validating assay sensitivity and specificity. This application extends to both cell-based and receptor-expressing membrane preparations, supporting the optimization of experimental protocols in drug discovery and receptor biology.
Endocrine feedback studies: The ability of this GnRH antagonist to acutely suppress pituitary gonadotropin output allows for precise manipulation of hormonal feedback loops in experimental models. Researchers use it to temporally control LH and FSH levels, thereby isolating and examining the contributions of upstream or downstream effectors in the hypothalamic-pituitary-gonadal axis. Such applications are instrumental in unraveling the dynamic interactions among hormones, receptors, and regulatory proteins involved in reproductive physiology.
Peptide synthesis and analytical reference: Owing to its well-characterized primary structure and bioactivity, Cetrorelix Acetate is employed as a reference standard in peptide synthesis and analytical method development. It serves as a benchmark for verifying peptide purity, sequence integrity, and chromatographic performance during the production and quality control of related peptide analogs. Analytical laboratories utilize the compound to calibrate instrumentation, validate detection methods, and ensure consistency in peptide-based research workflows, thereby supporting rigorous standards in peptide chemistry and bioanalytical applications.
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