Degarelix acetate is a synthetic peptide that acts as a gonadotrophin-releasing hormone (GnRH) antagonist. Degarelix, also known as FE-200486 and ASP-3550, is a long-acting, synthetic peptide with gonadotrophin-releasing hormone (GnRH) antagonistic properties. Degarelix targets and blocks GnRH receptors located on the surfaces of gonadotroph cells in the anterior pituitary, thereby reducing secretion of luteinizing hormone (LH) by pituitary gonadotroph cells and so decreasing testosterone production by interstitial (Leydig) cells in the testes.
CAT No: R1957
CAS No:934246-14-7
Synonyms/Alias:Degarelix acetate hydrate;934246-14-7;Firmagon;Degarelix acetate (USAN);Degarelix acetate [USAN];UNII-I18S89P20R;DEGARELIX ACETATE [MART.];I18S89P20R;N-ACETYL-3-(NAPHTHALEN-2-YL)-D-ALANYL-4-CHLORO-D-PHENYLALANYL-3-(PYRIDIN-3-YL)-D-ALANYL-L-SERYL-4-((((4S)-2,6-DIOXOHEXAHYDROPYRIMIDIN-4-YL)CARBONYL)AMINO)-L-PHENYLALANYL-4-(CARBAMOYLAMINO)-D-PHENYLALANYL-L-LEUCYL-N6-(1-METHYLETHYL)-L-LYSYL-L-PROLYL-D-ALANINAMIDE ACETATE HYDRATE;DEGARELIX ACETATE [WHO-DD];DEGARELIX ACETATE HYDRATE [MI];DEGARELIX ACETATE [ORANGE BOOK];D08635;Ac-2Nal-4Cpa-3Pal-Ser-4Aph(hydroorotyl)-4Aph(carbamoyl)-Leu-ILys-pro-Ala-NH2;
Chemical Name:(4S)-N-[4-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2R)-1-amino-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-6-(propan-2-ylamino)hexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[4-(carbamoylamino)phenyl]-1-oxopropan-2-yl]amino]-3-oxopropyl]phenyl]-2,6-dioxo-1,3-diazinane-4-carboxamide;acetic acid;hydrate
Degarelix Acetate Hydrate is a synthetic peptide compound that functions as a potent and selective gonadotropin-releasing hormone (GnRH) antagonist. Structurally engineered to mimic endogenous peptide sequences, it exhibits high affinity for the GnRH receptor, effectively blocking the receptor's activation and downstream hormonal signaling. Its unique biochemical profile, characterized by rapid onset of action and reversible suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion, has made it a valuable tool in endocrine research and hormone regulation studies. As a research-use-only peptide, Degarelix Acetate Hydrate provides a robust platform for investigating the physiological and molecular mechanisms of the hypothalamic-pituitary-gonadal axis across a range of experimental models.
Endocrine signaling research: Degarelix Acetate Hydrate is widely utilized in studies focused on the regulation of reproductive hormones and the broader endocrine system. By antagonizing GnRH receptors at the pituitary level, it enables precise, temporally controlled suppression of gonadotropin release. Researchers employ this compound to dissect the feedback mechanisms governing LH and FSH secretion, to clarify the roles of these hormones in reproductive physiology, and to explore the downstream impact on gonadal steroidogenesis in both in vitro and in vivo settings.
Hormone-dependent cancer modeling: The peptide's ability to induce rapid and reversible suppression of gonadotropins makes it a critical reagent in preclinical models of hormone-dependent cancers. In particular, it is used to simulate androgen deprivation in animal models, facilitating the study of tumor growth dynamics, resistance mechanisms, and the molecular consequences of hormonal manipulation. This application supports the development and validation of new therapeutic strategies targeting the hormonal axis in oncology research.
Peptide pharmacology and receptor binding studies: As a well-characterized GnRH antagonist, Degarelix Acetate Hydrate serves as a standard reference compound in receptor binding assays and pharmacodynamic profiling. Its defined mechanism of action allows researchers to benchmark novel GnRH analogues, assess receptor selectivity, and investigate structure-activity relationships. Such studies contribute to the rational design and optimization of next-generation peptide therapeutics targeting the GnRH pathway.
Reproductive physiology experimentation: The compound is instrumental in experimental protocols designed to modulate reproductive hormone levels for mechanistic studies. By providing a rapid and controllable means of suppressing endogenous gonadotropin secretion, it enables researchers to investigate the effects of hormonal ablation on spermatogenesis, ovarian function, and secondary sexual characteristics. These applications are essential for elucidating the complex interplay between the hypothalamus, pituitary, and gonads in vertebrate systems.
Peptide formulation and stability assessment: Degarelix Acetate Hydrate is also employed in the development and optimization of peptide drug delivery systems. Its physicochemical properties and sensitivity to formulation conditions make it a suitable candidate for evaluating the stability, solubility, and bioavailability of peptide-based pharmaceuticals. Studies using this compound help inform best practices for peptide storage, reconstitution, and administration in laboratory research environments, thereby supporting the advancement of peptide science and technology.
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More