Tiprelestat is a potent and selective inhibitor used in the biomedical industry. It targets neutrophil elastase, an enzyme involved in tissue inflammation and destruction. Tiprelestat helps reduce lung damage caused by excessive neutrophil activity, improving patient outcomes and promoting recovery.
CAT No: R1986
CAS No:820211-82-3
Chemical Name:(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(1R,4S,4aS,7S,7aS,10S,10aS,13aR,16S,20aS,22S,23aS,25S,26aS,28S,29aS,31S,32aS,34R,37S,40S,43S,46S,49S,52S,58R,63R,66S,72S,75R,81S,84S,87R,92R,98S)-58-[[(2S)-2-[[2-[[(2S)-1-[(2S)-6-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-aminopropanoyl]amino]-5-oxopentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-7a,10a,23a-tris(4-aminobutyl)-7,22-bis(2-amino-2-oxoethyl)-4a,40,46,49-tetrakis[(2S)-butan-2-yl]-4,37-bis(3-carbamimidamidopropyl)-66-(2-carboxyethyl)-26a,32a-bis(carboxymethyl)-29a-[(1R)-1-hydroxyethyl]-72-(hydroxymethyl)-31,84-dimethyl-20a,25,43-tris(2-methylpropyl)-28,81-bis(2-methylsulfanylethyl)-2a,3,5a,6,8a,9,11a,15,18a,21,21a,24,24a,27,27a,30,30a,33,33a,35a,36,39,42,45,48,51,57,64,67,70,73,76,79,82,85,93,99-heptatriacontaoxo-15a,16a,38a,39a,60,61,89,90-octathia-a,2,3a,5,6a,8,9a,12a,14,19a,20,22a,23,25a,26,28a,29,31a,32,34a,35,36a,38,41,44,47,50,56,65,68,71,74,77,80,83,86,94-heptatriacontazaoctacyclo[90.25.17.434,75.263,113.010,14.016,20.052,56.094,98]tetracontahectane-87-carbonyl]amino]-3-phenylpropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid
Tiprelestat is a small-molecule inhibitor recognized for its potent and selective activity against neutrophil elastase, a serine protease involved in the degradation of extracellular matrix components and modulation of inflammatory responses. As a non-peptidic, synthetic compound, tiprelestat has garnered significant interest in biochemical and pharmacological research owing to its capacity to modulate protease-driven pathways. Its chemical structure and mechanism of action make it a valuable tool for dissecting the roles of neutrophil elastase in various cellular and molecular contexts, particularly those related to inflammation, tissue remodeling, and protease regulation.
Enzyme inhibition studies: Tiprelestat serves as an essential reference compound for investigating the kinetics and specificity of serine protease inhibition, especially within the context of neutrophil elastase. By providing a well-characterized inhibitor, researchers can delineate the contribution of elastase to proteolytic cascades, validate assay systems, and benchmark novel inhibitory molecules. Its use enables precise quantification of enzyme activity modulation, supporting the development of robust screening platforms and mechanistic enzymology research.
Inflammation and immunology research: The compound is widely utilized in studies exploring the molecular mechanisms underlying inflammatory processes and immune cell regulation. By selectively targeting neutrophil elastase, tiprelestat allows for the dissection of protease-driven signaling pathways that influence cytokine release, leukocyte migration, and tissue injury. Such investigations are pivotal for understanding the interplay between proteases and immune mediators in both acute and chronic inflammatory models.
Pulmonary biology and tissue remodeling: Tiprelestat is frequently employed in experimental systems designed to model lung injury, fibrosis, and extracellular matrix turnover. Its inhibitory action facilitates the assessment of neutrophil elastase's impact on matrix protein degradation, epithelial barrier integrity, and fibroblast activation. These studies provide mechanistic insights into the processes that drive tissue remodeling and pulmonary dysfunction, thereby advancing the field of respiratory biology.
Biomarker validation and analytical assay development: The compound is a valuable tool in the development and optimization of analytical assays for detecting neutrophil elastase activity in biological samples. Its inclusion in assay validation protocols ensures specificity and sensitivity by serving as a positive control or reference inhibitor. This application is critical for biomarker research, particularly in the context of inflammatory diseases where neutrophil elastase serves as a potential diagnostic or prognostic indicator.
Drug discovery and structure-activity relationship studies: Tiprelestat's well-defined molecular scaffold makes it an important standard in medicinal chemistry efforts aimed at designing next-generation elastase inhibitors. Researchers utilize it to compare the efficacy, selectivity, and pharmacological profiles of new chemical entities. Its role in structure-activity relationship studies helps elucidate the structural determinants of protease inhibition, guiding the rational design of improved compounds for research and development pipelines.
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