Leuprolide acetate (Leuprorelin acetate) is a potent gonadotropin-releasing hormone receptor agonist used for the treatment of prostate cancer, endometriosis, uterine fibroids.
CAT No: 10-101-22
CAS No:74381-53-6
Synonyms/Alias:Leuprolide acetate;Leuprorelin acetate;Lupron;74381-53-6;Carcinil;Lucrin;Eligard;Enantone;Leuplin;Viadur;Lupron Depot;Abbott-43818;Prostap;TAP-144;Fensolvi;Leuprin;Lupaneta;Procrin;Trenantone;Leuplin depot;Lutrate depot;Procren Depot;Uno-Enantone;Depo-Lupron;LUPRON DEPOT-PED;Leuporelin acetate;Lupron PED;TAP-144-SR;Leuprolide Monoacetate;Enanton;Lutrate;Leuprolide acetate depot;LUPRON DEPOT-3;LUPRON DEPOT-4;Abbott 43818;CHEBI:63597;UNII-37JNS02E7V;37JNS02E7V;A-43818;Leuprolide (Acetate);DTXSID7049009;Leuprolide acetate [USAN:USP];DTXCID2028935;Leuprolide acetate [USAN];des-Gly10-[D-Leu6]-LH-RH ethylamide;Leuprolide acetate (USAN:USP);LEUPROLIDE ACETATE (USP-RS);LEUPROLIDE ACETATE [USP-RS];LEUPRORELIN ACETATE (MART.);LEUPRORELIN ACETATE [MART.];MFCD00072080;LEUPRORELIN ACETATE [JAN];LEUPROLIDE ACETATE (USP MONOGRAPH);LEUPROLIDE ACETATE [USP MONOGRAPH];Acetate, Leuprolide;LEUP;MFCD00167544;Ginecrin;Onectyl;Procren;Depo-Eligard;Enantone-Gyn;Fensolvi Kit;Lucrin Depot;Lupron Depot Ped;Leuprolide Acetate?;Lupron Depot-Ped Kit;ELIGARD KIT;Lupron Depot-3 Month;Lupron Depot-4 Month;LUTRATE DEPOT KIT;NCGC00183364-01;SCHEMBL3174;MLS000028695;CHEMBL1200775;LEUPROLIDE ACETATE [VANDF];LEUPROLIDE MONOACETATE [MI];Tox21_113507;BDBM50247891;LEUPRORELIN ACETATE [WHO-DD];s3718;AKOS015895632;AKOS030485977;CCG-270666;CS-1434;FL24877;LEUPROLIDE ACETATE [ORANGE BOOK];5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tryosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide monoacetate (salt);AC-28731;HY-13665;SMR000058945;CAS-74381-53-6;L0249;(Des-Gly10,D-Leu6,Pro-NHEt9)-LHRH acetate;Leuprolide Acetate (53714-56-0 free base);Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt.HOAc;Q27104908;PGLU-HIS-TRP-SER-TYR-D-LEU-LEU-ARG-PRO-NHC2H5 ACETATE SALT;5-OXO-L-PROLYL-L-HISTIDYL-L-TRYPTOPHYL-L-SERYL-L-TRYOSYL-D-LEUCYL-L-LEUCYL-L-ARGINYL-N-ETHYL-L-PROLINAMIDE ACETATE (SALT);5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tryosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide monoacetate;5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide--acetic acid (1/1);6-D-Leucine-9-(N-ethyl-L-prolinamide)-10-deglycinamideluteinizing hormone-releasing factor acetate;L-Prolinamide, 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-, acetate (1:1);
Leuprolide Acetate is a synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH), engineered to modulate the hypothalamic-pituitary-gonadal axis with high potency and specificity. Structurally modified for enhanced stability and receptor affinity, this peptide has become a fundamental tool in neuroendocrine research and hormone regulation studies. Its capacity to act as a GnRH agonist, coupled with its resistance to rapid enzymatic degradation, makes it an essential reagent for probing the molecular dynamics of reproductive signaling pathways, hormonal feedback mechanisms, and pituitary function. The compound's unique profile enables researchers to dissect the physiological and biochemical consequences of sustained GnRH receptor activation, providing insight into both fundamental biology and potential translational applications.
Endocrine Research: Leuprolide derivatives are extensively utilized in studies investigating the regulation of gonadotropin release and the downstream effects on sex steroid biosynthesis. By acting as a potent GnRH receptor agonist, the compound induces an initial surge in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion, followed by receptor desensitization and suppression of gonadotropin output upon prolonged exposure. Researchers employ this mechanism to model feedback inhibition, explore the regulation of reproductive hormones, and characterize the molecular events underlying pituitary-gonadal axis modulation in various species.
Reproductive Biology: In the context of reproductive physiology, leuprolide analogs serve as valuable probes for elucidating the hormonal control of gametogenesis and gonadal function. Their ability to manipulate endogenous hormone levels in vitro and in vivo enables detailed analysis of spermatogenesis, oogenesis, and steroidogenesis. Investigators leverage these properties to study the temporal dynamics of reproductive cycles, assess the impact of altered GnRH signaling on fertility, and dissect gene expression patterns responsive to hormonal cues.
Oncological Research Models: The compound is widely implemented in the development of experimental models that mimic hormone-dependent tumor environments. By modulating the endocrine milieu, leuprolide-based reagents facilitate the investigation of tumorigenesis, progression, and hormone responsiveness in cell culture and animal models. Such studies are instrumental in understanding the role of endocrine regulation in the proliferation and differentiation of hormone-sensitive tissues, as well as in identifying molecular targets for future intervention strategies.
Peptide Pharmacology: As a chemically stable GnRH analog, leuprolide serves as a reference molecule for structure-activity relationship (SAR) studies and the design of next-generation peptide therapeutics. Its defined sequence and receptor selectivity make it an ideal benchmark for evaluating modifications that influence peptide stability, receptor binding, and downstream signaling. Peptide chemists and pharmacologists use it to validate synthetic methodologies, optimize analog design, and benchmark new candidates in receptor activation assays.
Analytical Method Development: The unique physicochemical properties of leuprolide analogs are exploited in the calibration and validation of analytical techniques, such as high-performance liquid chromatography (HPLC) and mass spectrometry. These methods are essential for the quantification, purity assessment, and structural characterization of peptide drugs and research reagents. The compound's well-characterized chromatographic and spectrometric signatures provide a reliable standard for method optimization in peptide analysis, supporting quality control and research applications across the biochemical sciences.
3. Adipose tissue is a key organ for the beneficial effects of GLP-2 metabolic function
4. Implications of ligand-receptor binding kinetics on GLP-1R signalling
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