Ganirelix acetate (or diacetate) is an injectable competitive gonadotropin-releasing hormone antagonist (GnRH antagonist). It works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of LH and FSH.
CAT No: 10-101-61
CAS No:123246-29-7
Synonyms/Alias:Ganirelix;124904-93-4;Orgalutran;Antagon;Ganirelixum;123246-29-7;UNII-IX503L9WN0;IX503L9WN0;Ganirelixum [INN-Latin];CHEMBL1251;Ganirelix (INN);CID 16134406;GANIRELIX [INN];Ganirelixum (INN-Latin);D-Alaninamide, N-acetyl-3-(1-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N6-(bis(ethylamino)methylene)-D-lysyl-L-leucyl-N6-(bis(ethylamino)methylene)-L-lysyl-L-prolyl-;D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N6-[bis(ethylamino)methylene]-D-lysyl-L-leucyl-N6-[bis(ethylamino)methylene]-L-lysyl-L-prolyl-;Ganirelix [INN:BAN];Orgalutran (TN);D 24598;D-24598;GANIRELIX [MI];GANIRELIX [VANDF];GANIRELIX [WHO-DD];GANIRELIX [EMA EPAR];SCHEMBL19712192;H01CC01;CHEBI:135910;GJNXBNATEDXMAK-PFLSVRRQSA-N;DTXSID401027283;GLXC-26188;BDBM50102454;LHRH,N-Ac-2-Nal(1)-4-Cl-Phe(2)-3-Pal(3)-Et2-hArg(6,8)-AlaNH2(10)-;AT42442;DB06785;GnRH, N-Ac-2-Nal(1)-4-Cl-Phe(2)-3-Pal(3)-Et2-hArg(6,8)-AlaNH2(10)-;N-Ac-(2-naphthyl)Ala-2-(4-Cl-Phe)-3-(3-pyridinyl-Ala)-6,8-Et2-hArg-10-AlaNH2-LHRH;DA-63686;LHRH, N-acetyl-2-naphthylalanyl(1)-(4-chlorophenylalanyl)(2)-3-pyrdinylalanyl(3)-diethylhomoarginyl(6,8)-alaninamide(10)-;D08010;EN300-19652012;Q5521314;Ac-D-Nal-[D-(pCl)Phe]-D-Pal-Ser-Tyr-D-Har(Et2)-Leu-Har(Et2)-Pro-DAla-NH2;Ac-D-2Nal-D-Phe(4-Cl)-D-3Pal-Ser-Tyr-D-hArg(Et,Et)-Leu-hArg(Et,Et)-Pro-D-Ala-NH2 3 AcOH;
Chemical Name:(2S)-1-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(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-(4-hydroxyphenyl)propanoyl]amino]-6-[bis(ethylamino)methylideneamino]hexanoyl]amino]-4-methylpentanoyl]amino]-6-[bis(ethylamino)methylideneamino]hexanoyl]-N-[(2R)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
Ganirelix is a synthetic decapeptide that functions as a potent gonadotropin-releasing hormone (GnRH) antagonist, widely utilized in reproductive biology and endocrinology research. As a peptide-based molecule, it is structurally engineered to competitively inhibit endogenous GnRH receptors, thereby modulating the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary. Its precise mechanism of action and robust receptor affinity make it a valuable tool for dissecting the molecular pathways underlying reproductive hormone regulation, as well as for modeling endocrine feedback systems in a controlled laboratory setting.
Endocrine signaling studies: Ganirelix is extensively employed in research focused on elucidating the dynamics of the hypothalamic-pituitary-gonadal (HPG) axis. By selectively blocking GnRH receptor activation, it enables researchers to investigate the downstream effects of gonadotropin suppression on steroidogenesis, gametogenesis, and feedback regulation. This targeted inhibition is instrumental in clarifying the temporal and quantitative relationships between GnRH signaling and reproductive hormone output, advancing the understanding of endocrine system physiology.
Assisted reproduction research: In the context of assisted reproductive technology (ART) studies, Ganirelix serves as a model compound for synchronizing follicular development in vitro and in animal models. Its ability to prevent premature LH surges allows for precise control over ovulatory timing, facilitating the study of oocyte maturation, follicular dynamics, and the optimization of stimulation protocols. Such applications are critical for refining protocols in reproductive biology and for developing new approaches to fertility preservation and enhancement in research settings.
Peptide-receptor interaction analysis: Due to its well-characterized structure and receptor specificity, Ganirelix is frequently used in biochemical assays to probe GnRH receptor binding kinetics, affinity, and downstream signaling events. These studies provide insights into the molecular determinants of peptide-receptor interactions, supporting the development of novel GnRH analogs and antagonists with improved pharmacological profiles. Its use in competitive binding assays and receptor activation studies contributes to the broader field of peptide hormone research.
Signal transduction pathway mapping: The compound's capacity to modulate hormone secretion in a dose-dependent and reversible manner makes it ideal for mapping intracellular signaling cascades triggered by GnRH receptor engagement. By applying Ganirelix in cellular and tissue models, researchers can delineate the pathways involved in gonadotropin synthesis and release, dissecting the roles of second messengers, kinases, and transcription factors. This knowledge is fundamental for understanding the integration of hormonal signals at the cellular level.
Peptide synthesis and pharmacological profiling: As a synthetic decapeptide, Ganirelix is also utilized as a reference standard in peptide synthesis workflows and analytical validation. Its defined sequence and bioactivity profile serve as benchmarks for evaluating synthetic methodologies, purity assessment, and the characterization of structure-activity relationships among GnRH antagonists. Such applications are essential for quality control, method development, and comparative studies within the peptide research and pharmaceutical development communities.
Use of GnRH antagonists in patients with an a priori poor IVF prognosis results in predictably poor outcomes. Patients without factors predicting poor outcome have acceptable PRs. The pattern of E2 rise immediately after initiation of GnRH antagonists does not predict cycle outcome. Oral contraceptives can be successfully used to schedule antagonist-based IVF cycles but might increase the risk of cycle cancellation in some patient populations.
Shapiro, D. B., Mitchell-Leef, D., Carter, M., & Nagy, Z. P. (2005). Ganirelix acetate use in normal-and poor-prognosis patients and the impact of estradiol patterns. Fertility and sterility, 83(3), 666-670.
Elevated estradiol (E(2)) levels predispose to development of ovarian hyperstimulation syndrome (OHSS). Since GnRH antagonist is associated with a reduction in E(2) levels, we hypothesized that GnRH-antagonist treatment of women down-regulated with GnRH agonist who are at risk of OHSS might reduce E(2) levels and avoid cycle cancellation.
Gustofson, R. L., Segars, J. H., & Larsen, F. W. (2006). Ganirelix acetate causes a rapid reduction in estradiol levels without adversely affecting oocyte maturation in women pretreated with leuprolide acetate who are at risk of ovarian hyperstimulation syndrome. Human Reproduction, 21(11), 2830-2837.
Ganirelix is effective, safe, and well tolerated. Compared with leuprolide acetate, ganirelix therapy has a shorter duration and fewer injections but produces a similar pregnancy rate.
Fluker, M., Grifo, J., Leader, A., Levy, M., Meldrum, D., Muasher, S. J., ... & Shapiro, D. B. (2001). Efficacy and safety of ganirelix acetate versus leuprolide acetate in women undergoing controlled ovarian hyperstimulation. Fertility and sterility, 75(1), 38-45.
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