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 is a synthetic peptide analog of vasopressin, engineered to function as a selective vasopressin V1A receptor agonist. Structurally, it is characterized by targeted modifications that confer high affinity for the V1A receptor subtype, while minimizing activity at V2 and V1B receptors. This selectivity enables precise modulation of vascular tone and smooth muscle contractility in experimental systems. Due to its defined receptor specificity and peptide nature, selepressin is a valuable tool in studies investigating vasopressinergic signaling pathways, vascular physiology, and the pharmacological dissection of receptor-mediated responses.
Receptor pharmacology research: Selepressin is extensively utilized in receptor pharmacology to dissect the roles of vasopressin receptor subtypes in vascular tissues and other smooth muscle systems. By selectively activating V1A receptors, researchers can delineate the downstream signaling events associated with this pathway, such as phospholipase C activation, intracellular calcium mobilization, and smooth muscle contraction. Its use permits the isolation of V1A-mediated effects from those mediated by V2 or V1B receptors, providing clarity in mechanistic studies of vasopressinergic function.
Vascular physiology studies: The compound serves as a precise tool for investigating the regulation of vascular tone and blood vessel reactivity in ex vivo and in vitro models. Through its potent V1A agonist activity, selepressin enables controlled induction of vasoconstriction in isolated vessel preparations or perfused organ systems. Researchers employ it to explore the contributions of V1A receptor activation to blood pressure regulation, vascular resistance, and endothelial function under various experimental conditions.
Peptide signaling pathway analysis: As a synthetic peptide with high receptor selectivity, selepressin is well-suited for probing peptide-mediated signaling mechanisms in cellular and tissue-based assays. Its defined activity profile allows for the study of G protein-coupled receptor signaling cascades, including second messenger generation and downstream effector activation, in systems expressing vasopressin receptors. This facilitates the mapping of intracellular events specific to V1A receptor engagement and the identification of potential modulators or interacting proteins.
Pharmacological profiling and antagonist screening: Selepressin is frequently employed as a reference agonist in pharmacological profiling assays designed to evaluate the potency and selectivity of novel vasopressin receptor ligands. By establishing a baseline V1A-mediated response, it provides a benchmark against which the efficacy of candidate antagonists or inverse agonists can be measured. This application is particularly valuable in drug discovery programs seeking to develop new modulators of vasopressinergic signaling for research or industrial purposes.
Peptide synthesis and analytical method development: The unique sequence and well-characterized activity of selepressin make it a model compound for the development and validation of peptide synthesis protocols and analytical techniques. Laboratories engaged in solid-phase peptide synthesis, high-performance liquid chromatography (HPLC), or mass spectrometry often utilize selepressin as a standard to optimize purification strategies, assess peptide stability, and calibrate detection methods. Its predictable physicochemical properties and biological activity profile support method optimization and quality benchmarking in peptide research workflows.
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