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 Acetate, a synthetic decapeptide and potent gonadotropin-releasing hormone (GnRH) antagonist, is renowned for its ability to rapidly and reversibly suppress the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Engineered through advanced peptide synthesis techniques, Ganirelix exhibits high affinity for the GnRH receptor, enabling precise modulation of the hypothalamic-pituitary-gonadal axis. Its unique amino acid sequence confers exceptional receptor specificity and metabolic stability, making it a valuable tool in both basic research and specialized laboratory settings. The compound's rapid onset of action and short elimination half-life allow for flexible experimental designs, while its proven efficacy in disrupting endogenous GnRH signaling pathways has established it as a preferred GnRH antagonist in a variety of scientific investigations.
Reproductive Endocrinology Research: Ganirelix is extensively utilized in studies focused on elucidating the regulatory mechanisms of reproductive hormones. By selectively inhibiting GnRH receptor activation, researchers can precisely control pituitary gonadotropin release, facilitating investigations into the feedback loops and molecular pathways governing LH and FSH secretion. This targeted suppression enables the dissection of ovarian and testicular function, the study of folliculogenesis, and the exploration of gametogenesis under controlled hormonal environments. As a result, it provides critical insights into the neuroendocrine regulation of fertility and reproductive cycles in animal models and in vitro systems.
Assisted Reproductive Technology Model Systems: In the context of assisted reproductive technology (ART) research, Ganirelix acetate serves as a key reagent for developing and refining ovulation induction protocols. Its ability to prevent premature LH surges allows for the synchronization of follicular development, thereby improving the timing and yield of oocyte retrieval in experimental ART models. This application is instrumental in optimizing superovulation regimens, evaluating the efficacy of novel gonadotropin analogs, and assessing the impact of controlled ovarian hyperstimulation on reproductive outcomes in non-clinical studies.
Endocrine Disruption Studies: The use of GnRH antagonists such as Ganirelix is pivotal in environmental and toxicological research investigating endocrine-disrupting compounds. By establishing a controlled baseline of suppressed gonadotropin secretion, scientists can assess the direct and indirect effects of environmental toxins, pharmaceuticals, or dietary factors on the reproductive axis. This approach enables the identification of compounds that interfere with hormone synthesis, secretion, or receptor activity, thereby advancing our understanding of endocrine disruption mechanisms and potential risks to reproductive health.
Signal Transduction Pathway Analysis: Ganirelix provides a robust tool for dissecting GnRH receptor-mediated signal transduction pathways in pituitary and extrapituitary tissues. By blocking endogenous GnRH action, it allows researchers to delineate the downstream signaling cascades, including G-protein coupled receptor activation, second messenger systems, and gene expression profiles. Such studies are essential for mapping the molecular architecture of hormonal signaling networks and for identifying novel targets for pharmacological intervention in hormone-dependent processes.
Comparative Physiology and Evolutionary Biology: The application of Ganirelix extends to comparative studies exploring the evolution and diversity of reproductive endocrine systems across vertebrate species. By modulating GnRH signaling in different animal models, investigators can compare the conservation and divergence of hormonal control mechanisms, reproductive strategies, and pituitary-gonadal interactions. These insights contribute to a broader understanding of reproductive adaptation and the evolutionary pressures shaping endocrine regulation in diverse biological contexts.
In summary, Ganirelix acetate stands as a versatile and indispensable tool in the field of reproductive biology, endocrine research, and molecular signaling studies. Its precise mechanism of GnRH antagonism enables the controlled manipulation of hormonal pathways, thereby supporting a wide spectrum of scientific applications, from elucidating basic reproductive physiology to advancing environmental health research and evolutionary biology. The compound's unique properties facilitate innovative experimental designs and contribute significantly to the progress of hormone-related research endeavors.
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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