Rotigaptide, also called ZP-123, is a peptide analog, which has been shown to increase gap junction intercellular conductance in cardiac muscle cells. Gap junctions are protein channels that are responsible for conducting electrical impulses between cells in the heart to maintain normal rhythm.
CAT No: 10-101-55
CAS No:355151-12-1
Synonyms/Alias:Rotigaptide;355151-12-1;ZP-123;ZP-123 (ZEALAND);GAP (WYETH);UNII-GFA1W6KO7N;GFA1W6KO7N;Rotigaptide [USAN:INN];Rotigaptide [USAN];rotigaptida;GAP 484;GAP 486;ZP123;ZP 123;Rotigaptide (USAN);ROTIGAPTIDE [INN];(2R,4S)-1-[(2R)-1-[(2R)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]-N-[2-[[(2R)-1-[(2-amino-2-oxoethyl)amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]-4-hydroxypyrrolidine-2-carboxamide;Ac-d-Tyr-d-Pro-d-Hyp-Gly-d-Ala-Gly-NH2;Glycinamide, N-acetyl-D-tyrosyl-D-prolyl-(4S)-4-hydroxy-D-prolylglycyl-D-alanyl-;Dipeptide 9f [PMID 19175320];Dipeptide 9f (PMID 19175320);CHEMBL450656;rotigaptidum;GAP-486;(2R)-N-(carbamoylmethyl)-2-(2-(((2R,4S)-1-((2R)-1-((2R)-2-acetamido-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carbonyl)-4-hydroxypyrrolidin-2-yl)formamido)acetamido)propanamide;(2R)-N-(carbamoylmethyl)-2-(2-{[(2R,4S)-1-[(2R)-1-[(2R)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]-4-hydroxypyrrolidin-2-yl]formamido}acetamido)propanamide;(2R,4S)-1-((2R)-1-((2R)-2-acetamido-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carbonyl)-N-(2-(((2R)-1-((2-amino-2-oxoethyl)amino)-1-oxopropan-2-yl)amino)-2-oxoethyl)-4-hydroxypyrrolidine-2-carboxamide;ZP123 peptide;zp1-23;GTPL9214;DTXCID10111515;CHEBI:230093;Ac-Tyr-Pro-Hyp-Gly-Ala-Gly-NH2;AKOS040742576;DB13067;DA-67291;MS-30756;HY-106225;CS-0025346;NS00071051;D05767;G17110;Q7370547;acetyl-tyrosyl-prolyl-hydroxyprolyl-glycyl-alanyl-glycinamide;N-Acetyl-d-tyrosyl-d-prolyl-(4S)-4-hydroxy-d-prolylglycyl-d-alanylglycinamide;
Rotigaptide is a synthetic peptide compound recognized for its potent modulatory effects on gap junction intercellular communication, with particular specificity for connexin43 (Cx43) channels. As a member of the antiarrhythmic peptide family, it has garnered significant interest in the biochemical research community due to its ability to enhance gap junction conductance and stabilize cell-to-cell electrical coupling. Rotigaptide's unique mechanism of action has established it as a valuable tool for studying the regulation of intercellular signaling in excitable tissues, as well as for dissecting the molecular basis of connexin-mediated communication. Its application extends across multiple fields, including electrophysiology, cellular signaling, and peptide pharmacology, making it a versatile asset in advanced life science investigations.
Electrophysiological research: Rotigaptide is widely utilized in electrophysiological studies to probe the functional dynamics of gap junctions in cardiac and other excitable tissues. By modulating Cx43-mediated electrical coupling, it enables researchers to systematically investigate the impact of altered gap junction conductance on tissue excitability, impulse propagation, and arrhythmogenic potential. This peptide serves as a precise tool for dissecting the physiological and pathological consequences of gap junction modulation, supporting the elucidation of intercellular communication pathways that underlie coordinated tissue function.
Connexin biology studies: In the context of molecular cell biology, Rotigaptide is employed to explore the regulation, trafficking, and phosphorylation status of connexin proteins, particularly Cx43. Its ability to enhance gap junctional communication allows scientists to assess how changes in connexin functionality influence cellular homeostasis, tissue integrity, and response to stress. Such studies are instrumental in clarifying the biochemical mechanisms that govern connexin assembly, turnover, and gating, providing insights into both normal physiology and disease-associated remodeling.
Signal transduction analysis: The compound is instrumental in research aimed at understanding how intercellular communication via gap junctions affects downstream signal transduction pathways. By selectively increasing gap junction permeability, Rotigaptide facilitates the transfer of ions, metabolites, and second messengers between adjacent cells, enabling the analysis of coordinated cellular responses to various stimuli. This application is particularly valuable for investigating the role of synchronized signaling in tissue development, repair, and adaptation.
Peptide structure-activity relationship (SAR) investigations: As a synthetic peptide with well-characterized activity, Rotigaptide is frequently used in structure-activity relationship studies to delineate the molecular features required for gap junction modulation. Researchers leverage it as a reference compound to compare the efficacy and specificity of novel peptide analogs or modified constructs. Such investigations advance the rational design of next-generation gap junction modulators and contribute to the broader understanding of peptide-protein interactions within the connexin family.
Cardiac tissue modeling: Rotigaptide is incorporated into ex vivo and in vitro cardiac tissue models to simulate and assess the effects of enhanced gap junctional coupling on action potential propagation and arrhythmia susceptibility. Its application in engineered heart tissues, organotypic cultures, and multicellular preparations supports the development of more physiologically relevant models for basic research and preclinical assessment. Through its targeted modulation of intercellular connectivity, the peptide enables precise control over tissue-level electrical properties, facilitating high-resolution studies of cardiac electrophysiology and arrhythmogenesis.
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