D-Pro9-Cetrorelix incorporates a D-proline substitution that introduces pronounced conformational restriction at position 9. The change influences backbone curvature, proteolytic resistance, and receptor-contact geometry. Researchers examine its altered binding patterns relative to native cetrorelix. Applications include SAR exploration, peptide stabilization strategies, and structural-biology research.
CAT No: Z10-101-210
Synonyms/Alias:(R)-1-(((R)-2-((S)-2-((S)-2-((R)-2-((R)-2-((R)-2-acetamido-3-(naphthalen-2-yl)propanamido)-3-(4-chlorophenyl)propanamido)-3-(pyridin-3-yl)propanamido)-3-hydroxypropanamido)-3-(4-hydroxyphenyl)propanamido)-5-ureidopentanoyl)-L-leucyl-L-arginyl)-N-((R)-1-amino-1-oxopropan-2-yl)pyrrolidine-2-carboxamide; Ac-D-2-Nal-D-Phe (4-Cl)-D-3-Pal-Ser-Tyr-D-Cit-Leu-Arg-D-Pro-D-Ala-NH2;(R)-N-((R)-1-amino-1-oxopropan-2-yl)-1-((2S,5R,8S,11S,14R,17R,20R)-3-((S)-2-amino-4-methylpentanoyl)-17-(4-chlorobenzyl)-2-(3-guanidinopropyl)-8-(4-hydroxybenzyl)-11-(hydroxymethyl)-20-(naphthalen-2-ylmethyl)-4,7,10,13,16,19,22-heptaoxo-14-(pyridin-3-ylmethyl)-5-(3-ureidopropyl)-3,6,9,12,15,18,21-heptaazatricosan-1-oyl)pyrrolidine-2-carboxamide
D-Pro9-Cetrorelix is a synthetic decapeptide analog derived from cetrorelix, featuring a D-proline substitution at position nine. As a member of the gonadotropin-releasing hormone (GnRH) antagonist peptide family, it is structurally engineered to modulate the activity of the GnRH receptor with high specificity. The incorporation of D-amino acids, such as D-proline, enhances the peptide's resistance to enzymatic degradation, making it particularly valuable for studies requiring increased metabolic stability. D-Pro9-Cetrorelix is widely recognized in biochemical research for its utility in probing the mechanisms of hormone regulation and receptor-ligand interactions, as well as for its role as a reference compound in the development of novel peptide therapeutics and antagonists.
Receptor binding studies: D-Pro9-Cetrorelix is extensively employed in receptor binding assays to investigate the affinity and specificity of GnRH antagonists for their target receptors. The D-proline substitution confers unique conformational properties, enabling researchers to dissect the molecular determinants of receptor recognition and antagonism. By utilizing this peptide in competitive binding experiments, scientists can map critical residues involved in ligand-receptor interactions, facilitating a deeper understanding of GnRH receptor pharmacology and supporting the rational design of next-generation antagonists.
Peptide functional analysis: The compound serves as an important tool for functional studies examining the downstream effects of GnRH receptor blockade in various in vitro systems. Its ability to inhibit GnRH-mediated signaling pathways allows for precise modulation of hormone-driven cellular responses. Researchers leverage D-Pro9-Cetrorelix to characterize signal transduction cascades, assess the impact of antagonism on gene expression profiles, and delineate the cellular consequences of GnRH inhibition in pituitary or reproductive tissue models.
Peptide stability and metabolism research: The introduction of D-amino acids into peptide sequences is a well-established strategy for improving proteolytic stability. D-Pro9-Cetrorelix provides a robust model for evaluating the metabolic fate of modified peptides in biological matrices. By comparing its degradation kinetics to native analogs, scientists can gain valuable insights into the influence of stereochemistry on peptide half-life, inform strategies for enhancing the bioavailability of peptide-based molecules, and optimize lead compounds for research or industrial applications.
Structure-activity relationship (SAR) studies: As a structurally modified GnRH antagonist, D-Pro9-Cetrorelix is instrumental in SAR investigations aimed at elucidating the relationship between peptide sequence, conformation, and biological activity. The presence of D-proline at position nine enables systematic exploration of how specific amino acid substitutions affect receptor binding, antagonist potency, and overall pharmacological profile. These studies are critical for guiding the development of novel analogs with tailored properties for research or preclinical purposes.
Synthetic peptide reference standard: In peptide synthesis and analytical laboratories, D-Pro9-Cetrorelix is frequently used as a reference standard for method development, quality control, and comparative analysis. Its defined sequence and well-characterized properties make it suitable for validating chromatographic techniques, calibrating mass spectrometric assays, and benchmarking the performance of synthetic processes. By providing a reliable standard, it supports the reproducibility and accuracy of peptide research across diverse experimental workflows.
3. An Open-label, Single-center, Safety and Efficacy Study of Eyelash Polygrowth Factor Serum
4. The spatiotemporal control of signalling and trafficking of the GLP-1R
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