Selepressin (INN), also known as [Phe(2),Ile(3), Hgn(4),Orn(iPr)(8)]vasopressin) is a potent, highly selective, short-acting peptide full agonist of the vasopressin 1A receptor and analog of vasopressin which is under development by Ferring Pharmaceuticals for the treatment of vasodilatory hypotension in septic shock.
CAT No: 10-101-173
CAS No:876296-47-8
Synonyms/Alias:SELEPRESSIN;Fe202158;876296-47-8;Fe 202158;Selepressin [USAN:INN];Selepressin [INN];UNII-8P2T76M0SJ;selepresina;selepressine;8P2T76M0SJ;FE-202158;(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-amino-10-(4-amino-4-oxobutyl)-7-(2-amino-2-oxoethyl)-16-benzyl-13-[(2S)-butan-2-yl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxo-5-(propan-2-ylamino)pentan-2-yl]pyrrolidine-2-carboxamide;SELEPRESSIN [USAN];SELEPRESSIN [WHO-DD];Glycinamide, L-cysteinyl-L-phenylalanyl-L-isoleucyl-6-oxo-L-lysyl-L-asparaginyl-L-cysteinyl-L-prolyl-n5-(1-methylethyl)-L-ornithyl-, cyclic (1-6)-disulfide;CHEMBL1817709;DTXSID90236538;(2-L-PHENYLALANINE,3-L-ISOLEUCINE,4-(6-OXO-L-LYSINE), 8-(5-N-(PROPAN-2-YL)-L-ORNITHINE))HUMAN VASOPRESSIN;selepressinum;(2S)-1-((4R,7S,10S,13S,16S,19R)-19-amino-10-(4-amino-4-oxobutyl)-7-(2-amino-2-oxoethyl)-16-benzyl-13-((2S)-butan-2-yl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl)-N-((2S)-1-((2-amino-2-oxoethyl)amino)-1-oxo-5-(propan-2-ylamino)pentan-2-yl)pyrrolidine-2-carboxamide;SCHEMBL19712230;GTPL11454;DTXCID20159029;BDBM50350870;DB12495;HY-105239;CS-0025461;Q21098876;
Selepressin, also known as FE 202158, is a synthetic peptide analog of vasopressin designed to selectively target the vasopressin V1A receptor. Distinguished by its high specificity and stability, Selepressin has attracted considerable attention in both basic and applied scientific research. Its unique receptor selectivity enables researchers to investigate vasopressin-mediated signaling pathways without the confounding effects associated with non-selective agonists. As a tool compound, Selepressin supports the exploration of vascular tone regulation, fluid balance, and inflammatory response, making it a valuable asset in the study of cardiovascular and renal physiology. The peptide's robust pharmacological profile and synthetic accessibility further enhance its utility in experimental models, allowing for controlled investigations into the mechanisms underlying vascular dysfunction and systemic inflammation.
Cardiovascular Research: Selepressin provides an advanced platform for dissecting the molecular mechanisms governing vasoconstriction and vascular resistance. By selectively activating the V1A receptor, it enables precise modulation of blood vessel tone in preclinical models, facilitating the study of hemodynamic parameters under various physiological and pathophysiological conditions. Its application in vascular research helps elucidate the role of vasopressinergic signaling in blood pressure regulation, vascular permeability, and endothelial function, offering insights that are critical for developing novel therapeutic strategies for circulatory disorders.
Inflammatory Response Modulation: The peptide's ability to specifically target the V1A receptor presents unique opportunities for studying the interplay between vasopressin signaling and systemic inflammation. In experimental settings, Selepressin is employed to investigate how selective V1A activation influences cytokine release, leukocyte migration, and endothelial barrier integrity. Such studies are instrumental in advancing our understanding of the molecular drivers of inflammation, particularly in models of acute systemic inflammatory states, and may inform the identification of new molecular targets for anti-inflammatory interventions.
Renal Physiology Studies: Researchers utilize Selepressin to probe the effects of V1A receptor modulation on renal hemodynamics and water-electrolyte balance. Its selectivity allows for detailed analysis of renal vascular resistance, glomerular filtration rate, and sodium handling, independent of V2 receptor-mediated antidiuretic effects. These investigations are essential for clarifying the distinct contributions of vasopressin receptor subtypes to kidney function and for unraveling the complex regulatory networks involved in fluid homeostasis.
Vascular Permeability Investigations: As a selective V1A agonist, Selepressin is a powerful tool for examining the mechanisms controlling microvascular leakage and endothelial barrier function. Experimental models employing this peptide help delineate the signaling cascades that govern vascular permeability, particularly under conditions of stress or injury. Insights gained from such studies are foundational for understanding the pathogenesis of edema and tissue hypoperfusion, and for guiding the development of pharmacological agents aimed at preserving vascular integrity.
Drug Discovery and Mechanistic Studies: The use of Selepressin extends to early-phase drug discovery programs and mechanistic explorations of peptide-receptor interactions. Its well-characterized receptor selectivity and pharmacodynamic profile make it an ideal reference compound for screening novel V1A-targeted agents or for benchmarking the efficacy of emerging therapeutic candidates. Additionally, it serves as a valuable molecular probe in structure-activity relationship studies, supporting rational drug design and the identification of lead compounds with improved specificity and safety profiles.
In summary, Selepressin's distinctive pharmacological properties and receptor selectivity underpin its broad utility in scientific research. From cardiovascular and renal physiology to inflammation and vascular barrier studies, this synthetic peptide analog enables precise experimental manipulation of vasopressin signaling pathways. Its role in drug discovery further highlights its value as a reference agent and mechanistic tool, supporting innovation and knowledge advancement across multiple domains of biomedical investigation.
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