Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
CAT No: 10-101-206
CAS No:115150-59-9
Synonyms/Alias:Antagonist G;115150-59-9;(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]-methylamino]-3-phenylpropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]-4-methylpentanamide;L-Methioninamide, L-arginyl-D-tryptophyl-N-methyl-L-phenylalanyl-D-tryptophyl-L-leucyl-;antagonist-g;RWFWLM;RW-N(Me)F-Wlm-NH2;Arg-trp-N-methyl-phe-trp-leu-met-NH2;H-Arg-D-trp-N(Me)phe-D-trp-leu-met-NH2;an-tagonist g;Antagonist G?;Arginyl-tryptophyl-N-methylphenylalanyl-tryptophyl-leucyl-methioninamide;L-Arginyl-O-tryptophyl-N-methyl-L-phenylalanyl-D-tryptophyl-L-leucyl-L-methioninamide;(Arg6,D-Trp7.9,N-Me-Phe8)-Substance P (6-11);CHEMBL4303227;HY-P1185;MFCD00133831;AKOS024456877;L-Methioninamide, L-arginyl-O-tryptophyl-N-methyl-L-phenylalanyl-D-tryptophyl-L-leucyl-;DA-59542;MS-31778;CS-0028917;ARG-D-TRP-N-ME-PHE-D-TRP-LEU-MET-NH2;G12365;(Arg6,D-Trp7?9,N-Me-Phe8)-Substance P (6-11);BRD-K25863791-001-01-8;(S)-N-((5S,8S,11R,14S,17R)-11-((1H-indol-3-yl)methyl)-14-benzyl-5-carbamoyl-18-(1H-indol-3-yl)-8-isobutyl-15-methyl-7,10,13,16-tetraoxo-2-thia-6,9,12,15-tetraazaoctadecan-17-yl)-2-amino-5-guanidinopentanamide;
Antagonist G is a synthetic peptide compound designed to selectively inhibit the activity of specific G protein-coupled receptor (GPCR) pathways. As a structurally defined peptide antagonist, it interferes with receptor-ligand interactions, enabling researchers to dissect complex signal transduction mechanisms in various biological systems. Its sequence and conformational properties allow for targeted modulation of GPCR-mediated responses, making it a valuable tool in biochemical, pharmacological, and molecular biology research. The ability to precisely block receptor activation provides significant utility in studies aiming to unravel the physiological and pathophysiological roles of GPCRs, which are central to numerous cellular processes.
Receptor signaling studies: Antagonist G is widely utilized to investigate the functional roles of specific GPCR subtypes in cellular signaling networks. By competitively inhibiting endogenous ligand binding, it enables researchers to delineate the contribution of individual receptors to downstream signaling events such as second messenger production, kinase activation, and gene transcription. This targeted inhibition is instrumental in mapping receptor-specific signaling cascades, facilitating a deeper understanding of cellular communication and regulatory mechanisms.
Pharmacological profiling: The peptide antagonist serves as an essential reagent in the pharmacological characterization of novel ligands and drug candidates targeting GPCRs. Through its selective blocking activity, it provides a reference point for evaluating the potency, selectivity, and efficacy of agonists and antagonists in both in vitro and ex vivo systems. Its use in dose-response and competition assays supports the identification of ligand-receptor interactions, aiding in the optimization of lead compounds during drug discovery and development.
Functional genomics: Antagonist G is employed in functional genomics experiments to assess the phenotypic consequences of acute GPCR inhibition in various cell types or model organisms. By transiently blocking receptor activity, researchers can observe alterations in cellular behavior, gene expression profiles, and physiological outputs. These insights are critical for elucidating gene function, understanding receptor-mediated signaling networks, and identifying potential targets for further investigation.
Peptide structure-activity relationship (SAR) analysis: The defined sequence and inhibitory properties of Antagonist G make it a valuable tool for structure-activity relationship studies in peptide research. Modifications to its amino acid composition or conformation can be systematically explored to determine the structural features essential for receptor binding and antagonistic activity. Such SAR investigations inform the rational design of next-generation peptide modulators with improved selectivity, potency, or stability.
Cellular assay development: In the context of assay development, the peptide antagonist is frequently incorporated into cell-based models to establish negative controls or baseline responses for GPCR activation studies. Its reliable inhibitory action ensures robust assay validation, enabling accurate quantification of receptor-mediated effects and minimizing background signaling. The use of Antagonist G in these systems enhances the reproducibility and interpretability of experimental results, supporting high-throughput screening and mechanistic investigations in academic and industrial laboratories.
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