Lonodelestat is a peptide analog constructed from aromatic, hydrophobic, and polar residues arranged to promote structured folding and surface interactions. Researchers use it to examine ligand-protein binding, secondary-structure transitions, and conformational energetics. Its balanced composition suits advanced biophysical analysis.
CAT No: R2420
CAS No:906547-89-5
Synonyms/Alias:Lonodelestat;Lonodelestat [INN];5SD2VOV3MF;906547-89-5;UNII-5SD2VOV3MF;POL6014;1,13-Anhydro(L-alanyl-L-seryl-L-isoleucyl-L-prolyl-lprolyl-L-glutaminyl-L-lysyl-L-tyrosyl-D-prolyl-L-prolyl-(2S)-2-aminodecanoyl-L-alpha-glutamyl-L-threonine);Cyclo(L-alanyl-L-seryl-L-isoleucyl-L-prolyl-L-prolyl-L-glutaminyl-L-lysyl-L-tyrosyl-D-prolyl-L-prolyl-(2S)-2-aminodecanoyl-L-alpha-glutamyl-L-threonyl);cyclo[Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-D-Pro-Pro-Nle(Bu)-Glu-Thr];1,13-ANHYDRO(L-ALANYL-L-SERYL-L-ISOLEUCYL-L-PROLYL-LPROLYL-L-GLUTAMINYL-L-LYSYL-L-TYROSYL-D-PROLYL-L-PROLYL-(2S)-2-AMINODECANOYL-L-.ALPHA.-GLUTAMYL-L-THREONINE);CYCLO(L-ALANYL-L-SERYL-L-ISOLEUCYL-L-PROLYL-L-PROLYL-L-GLUTAMINYL-L-LYSYL-L-TYROSYL-D-PROLYL-L-PROLYL-(2S)-2-AMINODECANOYL-L-.ALPHA.-GLUTAMYL-L-THREONYL);cyclo(Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-D-Pro-Pro-Nle(Bu)-Glu-Thr);GTPL11275;HY-P3293;POL-6014;AKOS040758444;DA-65052;CS-0204184;Cyclo[L-alanyl-L-seryl-L-isoleucyl-L-prolyl-L-prolyl-L-glutaminyl-L-lysyl-L-tyrosyl-D-prolyl-L-prolyl-(2S)-2-aminodecanoyl-L-alpha-glutamyl-L-threonyl] (9CI);
Lonodelestat, also known as BAY 39-9437 or POL6014, is a synthetic small molecule inhibitor specifically designed to target human neutrophil elastase (HNE). As a potent and selective inhibitor, Lonodelestat is distinguished by its ability to modulate the activity of neutrophil elastase, an enzyme implicated in a range of inflammatory and tissue-destructive processes. Its chemical structure allows for high specificity, making it a valuable tool in biochemical and cellular research focused on neutrophil function, protease regulation, and inflammatory mechanisms. The compound's stability and solubility characteristics further enhance its utility in both in vitro and in vivo experimental systems, supporting a broad spectrum of investigative applications in the life sciences.
Inflammation Research Models: Lonodelestat is widely utilized in inflammation research to explore the role of neutrophil elastase in acute and chronic inflammatory responses. By selectively inhibiting elastase activity, researchers can dissect the enzyme's contribution to the recruitment and activation of immune cells, cytokine release, and tissue remodeling. This approach enables the elucidation of underlying mechanisms driving inflammatory diseases and facilitates the identification of novel therapeutic targets within the inflammatory cascade. The use of Lonodelestat in cellular and animal models provides critical insight into how modulation of elastase activity influences disease progression and resolution.
Pulmonary Disease Mechanism Studies: Lonodelestat serves as an indispensable reagent in studies investigating the pathophysiology of pulmonary diseases characterized by excessive neutrophil infiltration and protease-mediated tissue damage. In experimental models of conditions such as cystic fibrosis, chronic obstructive pulmonary disease (COPD), and acute lung injury, inhibition of neutrophil elastase by this compound allows researchers to examine the downstream effects on mucus viscosity, airway remodeling, and epithelial barrier integrity. These studies contribute to a deeper understanding of the molecular drivers of lung dysfunction and support the development of strategies aimed at preserving pulmonary architecture and function.
Protease Pathway Elucidation: The use of Lonodelestat extends to the broader study of protease networks and their regulation in various biological systems. By providing a means to selectively block elastase activity, scientists can differentiate the specific roles of neutrophil elastase from other serine proteases, such as proteinase 3 or cathepsin G, within complex proteolytic cascades. This specificity aids in mapping substrate preferences, identifying endogenous inhibitors, and characterizing feedback mechanisms that maintain proteolytic balance in tissues. The insights gained from such studies are vital for advancing knowledge of protease-mediated signaling and tissue homeostasis.
Drug Discovery and Screening: In the context of pharmaceutical research, Lonodelestat is frequently employed as a reference compound or tool molecule in drug screening assays targeting neutrophil elastase or related proteases. Its well-characterized inhibitory profile makes it an ideal standard for evaluating the potency, selectivity, and efficacy of novel elastase inhibitors. Moreover, the compound's utility in high-throughput screening platforms accelerates the identification of promising drug candidates and informs structure-activity relationship studies, ultimately supporting the optimization of new chemical entities for further preclinical development.
Ex Vivo and Translational Research: Lonodelestat also plays a significant role in ex vivo studies using human tissue samples or organotypic cultures, where it is used to assess the impact of neutrophil elastase inhibition on tissue injury, inflammatory mediator release, and cellular responses. These translational research applications bridge the gap between basic mechanistic studies and clinical investigation by providing relevant data on the modulation of disease processes in human-derived systems. The insights generated from such work inform the rational design of intervention strategies and enhance the predictive value of preclinical research for human health.
Lonodelestat stands as a versatile and scientifically valuable compound for advancing research into neutrophil elastase biology, inflammatory mechanisms, pulmonary disease processes, protease regulation, and drug discovery. Its selective inhibitory action, combined with favorable experimental properties, enables researchers to address fundamental questions in immunology, respiratory science, and translational medicine. As the understanding of protease-driven pathology continues to evolve, Lonodelestat remains an essential tool for dissecting complex biological pathways, validating new therapeutic targets, and supporting the progression of innovative research across diverse biomedical disciplines.
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