Desirudin is a synthetic recombinant form of the naturally occurring hirudin, the anticoagulant substance found in leech. Desirudin is a selective and almost irreversible inhibitor of thrombin, both free and clot-bound, by blocking its active site. This anticoagulant agent has no effect on other components of the hemostatic system. Desirudin is particularly used to prevent deep vein thrombosis in patients undergoing hip and knee replacement surgery.
CAT No: 10-101-340
CAS No:120993-53-5
Synonyms/Alias:Desirudin;120993-53-5;CGP 39393;CGP-39393;IK-HIR02;Revasc;UNII-U0JZ726775;63-Desulfohirudin (Hirudo medicinalis isoform HV1);DTXSID90153094;CGP39393;U0JZ726775;recombinant HV1 hirudin;Desirudin [USAN:INN:BAN];Hirudin desirudin;63-Desulfohirudin;DESIRUDIN (MART.);GTPL6458;DTXCID9075585;Hirudin (Hirudo medicinalis isoform HV1), 63-desulfo-;63-Desulfohirudin (recombinant);B01AE01;DA-52459;63-Desulfohirudin(Hirudo medicinalis isoform HV1);
Chemical Name:(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S,3R)-2-[[(2S)-2-[[(1R,6R,9S,12S,15S,18S,24S,27S,33S,36S,39R,44R,47S,53S,56S,59S,67S,73S,76S)-15,76-bis(4-aminobutyl)-44-[[(2S)-2-[[(4R,7S,10S,13S,19S,22S,25S,28R)-28-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-10-(2-amino-2-oxoethyl)-13-(3-amino-3-oxopropyl)-22-(2-carboxyethyl)-25-[(1R)-1-hydroxyethyl]-19-(hydroxymethyl)-7-(2-methylpropyl)-6,9,12,15,18,21,24,27-octaoxo-1,2-dithia-5,8,11,14,17,20,23,26-octazacyclononacosane-4-carbonyl]amino]-4-methylpentanoyl]amino]-12,56,73-tris(2-amino-2-oxoethyl)-9,67-bis(3-amino-3-oxopropyl)-36-[(2S)-butan-2-yl]-18,47-bis(2-carboxyethyl)-24-(carboxymethyl)-27,53-bis(hydroxymethyl)-33-(2-methylpropyl)-8,11,14,17,20,23,26,29,32,35,38,45,48,51,54,57,60,62,65,68,71,74,77-tricosaoxo-59-propan-2-yl-3,4,41,42-tetrathia-7,10,13,16,19,22,25,28,31,34,37,46,49,52,55,58,61,63,66,69,72,75,78-tricosazabicyclo[37.22.17]octaheptacontane-6-carbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-3-carboxypropanoyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoic acid
Desirudin, also known as recombinant hirudin, is a highly specific and potent direct thrombin inhibitor derived from the medicinal leech Hirudo medicinalis. As a synthetic polypeptide, Desirudin exhibits exceptional stability and reproducibility, making it a valuable tool for researchers studying coagulation pathways and thrombin-mediated processes. Its unique structure enables it to bind both the active site and exosite of thrombin, thereby preventing the conversion of fibrinogen to fibrin and inhibiting clot formation. The recombinant production of Desirudin ensures batch-to-batch consistency, which is essential for experimental reliability and reproducibility in laboratory settings. Its application extends across a wide spectrum of biochemical and physiological studies, particularly those focused on hemostasis, thrombosis, and vascular biology.
Coagulation Research: Desirudin is extensively utilized in the investigation of blood coagulation mechanisms. By providing a highly selective and reversible inhibition of thrombin, it allows scientists to dissect the roles of thrombin in the coagulation cascade and to study the interplay between various coagulation factors. Its use in in vitro plasma or whole blood assays enables researchers to model thrombin inhibition and analyze downstream effects on clot formation, platelet activation, and fibrinolysis. This facilitates a deeper understanding of hemostatic balance and the molecular underpinnings of coagulation disorders, supporting the development of novel therapeutic targets and strategies.
Thrombosis Modeling: In the context of thrombosis research, recombinant hirudin serves as an indispensable agent for modeling and modulating thrombotic events in experimental systems. Researchers employ it to inhibit thrombin activity in animal models or ex vivo systems, helping to elucidate the pathophysiology of thrombus formation and propagation. Its precise action enables the study of antithrombotic interventions and the evaluation of new anticoagulant compounds, providing a robust platform for preclinical investigation of thrombosis-related disorders.
Vascular Biology Studies: Desirudin's capacity to modulate thrombin-mediated cellular responses makes it a powerful tool in vascular biology. Thrombin not only catalyzes fibrin formation but also activates endothelial cells and smooth muscle cells, influencing vascular tone, permeability, and inflammation. By selectively inhibiting thrombin, Desirudin allows researchers to isolate and analyze the specific contributions of thrombin signaling to vascular remodeling, angiogenesis, and endothelial dysfunction. These insights are crucial for advancing the understanding of vascular pathologies and for developing targeted interventions to mitigate vascular damage.
Platelet Function Analysis: The role of Desirudin in platelet function studies is significant, as thrombin is a potent activator of platelets. By blocking thrombin's interaction with platelet receptors, it enables the assessment of platelet aggregation and activation independent of thrombin's effects. This is particularly valuable in dissecting the contributions of other agonists and signaling pathways in platelet biology. Such research supports the identification of new antiplatelet strategies and enhances knowledge of platelet involvement in hemostatic and thrombotic processes.
Biochemical Assays and Drug Screening: The specificity and stability of recombinant hirudin make it an ideal reagent for biochemical assays that require precise control of thrombin activity. It is frequently incorporated into enzyme assays, chromogenic substrate tests, and high-throughput screening platforms to evaluate the inhibitory potential of candidate molecules or to standardize assay conditions. Its use ensures reproducibility and accuracy in measuring thrombin-dependent reactions, thus supporting the discovery and optimization of novel anticoagulant agents and other therapeutics targeting the coagulation cascade.
In summary, Desirudin stands as a versatile and scientifically valuable polypeptide for a broad array of research applications. Its role in coagulation research, thrombosis modeling, vascular biology studies, platelet function analysis, and biochemical assay development underscores its importance as a tool for advancing fundamental and translational research in hemostasis and vascular science. By enabling precise modulation of thrombin activity, it continues to facilitate new discoveries and the development of innovative approaches to understanding and addressing disorders of coagulation and vascular function.
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