(D-His2)-Leuprolide Trifluoroacetic Acid Salt features a stereochemical substitution at position two, modifying receptor-contact geometry and backbone folding. The peptide's aromatic and charged residues support structural studies of ligand dynamics. Researchers employ it to investigate conformation-driven recognition and helix formation. Its TFA form improves solubility and handling.
CAT No: R2262
CAS No:112642-11-2
Synonyms/Alias:12642-11-2;(D-His2)-Leuprolide Trifluoroacetic Acid Salt;(Des-Gly10,D-His2,D-Leu6,Pro-NHEt9)-LHRH;MFCD02264520;D-HIS-LEUPROLIDE;TN3XE824EM;FD109240;(Des-Gly10,D-His2,D-Leu6,Pro-NHEt 9)-LHRH;Pyr-D-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt; pE-(dH)WSY(dL)LRP-NHEt;5-OXO-L-PROLYL-D-HISTIDYL-L-TRYPTOPHYL-L-SERYL-L-TYROSYL-D-LEUCYL-L-LEUCYL-L-ARGINYL-N-ETHYL-L-PROLINAMIDE; (S)-1-((3R,6S,9S,12S,15R,18S,21S)-3-((1H-imidazol-5-yl)methyl)-6-((1H-indol-3-yl)methyl)-21-(3-guanidinopropyl)-12-(4-hydroxybenzyl)-9-(hydroxymethyl)-15,18-diisobutyl-1,4,7,10,13,16,19-heptaoxo-1-((S)-5-oxopyrrolidin-2-yl)-2,5,8,11,14,17,20-heptaazadocosan-22-oyl)-N-ethylpyrrolidine-2-carboxamide; (D-His2)-Leuprolide
(D-His2)-Leuprolide Trifluoroacetic Acid Salt is a specialized synthetic peptide derivative designed for advanced research applications in the fields of biochemistry, endocrinology, and molecular biology. As a modified analog of leuprolide, this compound incorporates a D-histidine substitution at the second amino acid position, which can significantly influence its binding characteristics and resistance to enzymatic degradation. The trifluoroacetic acid salt form enhances its solubility and stability, making it particularly suitable for use in aqueous solutions and complex biological assays. Researchers value this analog for its ability to interact with gonadotropin-releasing hormone (GnRH) receptors, offering a versatile platform for studying receptor-ligand dynamics and peptide-based modulation of hormonal pathways. Its well-defined structure and consistent quality facilitate reproducible results, supporting a wide range of experimental designs and investigative approaches.
Endocrine Signaling Pathway Analysis: In the context of endocrine research, (D-His2)-Leuprolide Trifluoroacetic Acid Salt serves as a valuable tool for dissecting the mechanisms of GnRH receptor activation and downstream signaling events. By introducing the D-histidine modification, scientists can examine how structural variations affect receptor selectivity, agonist potency, and desensitization processes. This enables detailed mapping of hormonal feedback loops and the evaluation of peptide analogs in modulating luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion in in vitro models. The compound's enhanced stability further allows for extended incubation periods and time-course studies, providing deeper insights into the temporal aspects of endocrine signaling.
Peptide Structure-Activity Relationship Studies: The unique configuration of this leuprolide analog makes it an excellent candidate for structure-activity relationship (SAR) investigations. Researchers utilize (D-His2)-Leuprolide derivatives to systematically compare the biological activities of natural and modified peptides, identifying critical residues responsible for receptor binding and functional selectivity. By exploring how the D-histidine substitution influences conformational dynamics and receptor affinity, scientists can design next-generation peptide therapeutics or molecular probes with improved efficacy and specificity. Such studies are fundamental for advancing peptide drug discovery and optimizing lead compounds in preclinical research settings.
Receptor Binding Assays and Ligand Screening: The high affinity and selectivity of (D-His2)-Leuprolide Trifluoroacetic Acid Salt for GnRH receptors make it a preferred standard in competitive binding assays and ligand screening platforms. Its use in radioligand displacement or fluorescence-based assays enables the quantification of receptor occupancy, binding kinetics, and antagonist interactions. These applications are critical for validating new receptor modulators, characterizing the pharmacological profiles of novel compounds, and elucidating the molecular basis of receptor-ligand recognition. The compound's stability and solubility contribute to robust assay performance and reproducibility across different experimental formats.
Cellular Signaling and Functional Assays: In cellular models, this peptide analog is employed to initiate or inhibit specific signaling cascades linked to GnRH receptor activation. Researchers can monitor downstream effects such as second messenger generation, transcriptional regulation, and cell proliferation using a variety of biochemical and molecular techniques. The D-histidine modification may confer altered resistance to proteolytic enzymes, allowing for prolonged stimulation or inhibition in cell-based assays. These attributes make it a versatile reagent for exploring the physiological and pharmacological consequences of modulating GnRH pathways in diverse cellular contexts.
Peptide Delivery and Formulation Research: Beyond its direct biological activities, (D-His2)-Leuprolide Trifluoroacetic Acid Salt is also utilized in studies focused on peptide delivery systems and formulation optimization. Investigators assess its compatibility with various carriers, encapsulation methods, and sustained-release technologies to enhance peptide bioavailability and stability. Insights gained from these studies support the development of innovative delivery platforms for peptide therapeutics and expand the toolkit for translational research in peptide-based drug design. By leveraging the unique properties of this analog, scientists can address challenges related to peptide solubility, degradation, and targeted delivery, ultimately contributing to the advancement of peptide science.
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