Bivalirudin is a DTI that overcomes many limitations seen with indirect thrombin inhibitors. It is a short, synthetic peptide that is potent, highly specific, and a reversible inhibitor of thrombin. Bivalirudin inhibits both circulating and clot-bound thrombin, while also inhibiting thrombin-mediated platelet activation and aggregation. It has a quick onset of action and a short half-life, without binding to plasma proteins (other than thrombin) or red blood cells. Therefore it has a predictable antithrombotic response.
CAT No: 10-101-06
CAS No:128270-60-0 (net)
Synonyms/Alias:BG 8967; Hirulog; Hirulog I; Bivalirudin; Angiomax; Hirulog-1; Hirulog1; Hirulog 1; BG8967; BG 8967; BG-8967; LS-172701; LS172701; LS 172701
Chemical Name:2-[[2-[[2-[[2-[[1-[(2S)-2-[[2-[[2-[[2-[[2-[[2-[[4-amino-2-[[2-[[2-[[2-[[2-[[1-[2-[[1-(2-amino-3-phenylpropanoyl)pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]-4-oxobutanoyl]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-methylpentanoic acid
Bivalirudin Trifluoroacetate is a synthetic peptide-based anticoagulant that functions as a direct thrombin inhibitor. Structurally derived from hirudin, it comprises a specific amino acid sequence that enables high-affinity binding to both the catalytic and anion-binding exosites of thrombin. This dual-site interaction underpins its ability to effectively inhibit thrombin-mediated processes, positioning it as a valuable tool for investigating coagulation pathways, thrombogenesis, and protease-substrate interactions within the broader fields of hematology, cardiovascular research, and peptide pharmacology. Its well-characterized mechanism of action and peptide nature make it particularly suitable for applications that require precise modulation of thrombin activity in vitro.
Coagulation Pathway Research: Bivalirudin Trifluoroacetate is extensively utilized in the study of coagulation cascades, providing researchers with a reliable means to selectively inhibit thrombin during biochemical assays. By directly blocking thrombin's activity, it allows for the dissection of individual steps in the clotting process, facilitating a deeper understanding of fibrin formation, platelet activation, and feedback regulation within the coagulation system. This specificity is especially valuable for elucidating the mechanistic roles of thrombin in both physiological hemostasis and pathological thrombosis.
Enzyme Kinetics and Inhibition Studies: The compound serves as a model direct thrombin inhibitor for kinetic analyses and inhibition profiling in enzymology. Its defined peptide sequence and reversible binding properties enable detailed characterization of thrombin's catalytic parameters, including substrate turnover rates and inhibitor binding constants. Researchers employ it to benchmark new anticoagulant candidates, validate assay platforms, and explore structure-activity relationships in serine protease inhibition.
Peptide-Protein Interaction Analysis: As a synthetic peptide, Bivalirudin Trifluoroacetate is instrumental in studies focusing on peptide-mediated modulation of protein targets. Its interaction with thrombin provides a robust system for examining the structural determinants of peptide-protein binding, allosteric regulation, and competitive inhibition. Such investigations contribute to the broader understanding of peptide therapeutics, protein engineering, and rational drug design targeting serine proteases.
Analytical Assay Development: The compound is frequently incorporated into in vitro assay systems designed to measure thrombin activity, screen for anticoagulant compounds, or validate diagnostic reagents for coagulation studies. Its consistent inhibitory profile and well-documented mechanism facilitate the standardization and calibration of chromogenic, fluorogenic, or clot-based assays, ensuring reproducibility and accuracy in experimental workflows across academic and industrial laboratories.
Peptide Synthesis and Modification Studies: The well-defined sequence of Bivalirudin Trifluoroacetate makes it a reference compound in peptide synthesis research and analytical method development. It is used to optimize solid-phase peptide synthesis protocols, assess peptide purity by HPLC or mass spectrometry, and evaluate strategies for peptide stabilization or functional modification. These applications support advancements in peptide chemistry, quality control, and the development of next-generation peptide-based research tools.
Growing data demonstrate procedural success with bivalirudin in patients with HIT undergoing cardiovascular surgery. However, bivalirudin dosing and goal-activated clotting times varied between the studies and case reports. Bivalirudin represents a viable alternative to heparin in patients with HIT undergoing cardiovascular surgery; however, further trials are warranted to identify optimal dosing and monitoring parameters.
Czosnowski Q A, Finks S W, Rogers K C. Bivalirudin for patients with heparin-induced thrombocytopenia undergoing cardiovascular surgery[J]. Annals of Pharmacotherapy, 2008, 42(9): 1304-1309.
Among the current agents in the class of direct thrombin inhibitors, bivalirudin has seen increased use in cardiovascular medicine over the past decade through its primary indication as an anticoagulant used during percutaneous coronary interventions. Bivalirudin has been further investigated and used as the anticoagulation strategy in the setting of cardiac and endovascular surgical procedures and is frequently utilized in the management of patients with heparin-induced thrombocytopenia. In comparison with heparin, bivalirudin exhibits a low immunogenic profile and provides similar or reduced major bleeding rates as well as a predictable degree of anticoagulation that is dose related. Bivalirudin primarily undergoes dual elimination via proteolytic cleavage and renal elimination, and requires dose adjustment in the setting of severe renal dysfunction. Given the body of supportive data, bivalirudin is likely to continue to figure prominently as a reliable and efficient anticoagulation strategy. Additional agents in the class of direct thrombin inhibitors are under investigation and may find increasing clinical use.
Van De Car D A, Rao S V, Ohman E M. Bivalirudin: a review of the pharmacology and clinical application[J]. Expert review of cardiovascular therapy, 2010, 8(12): 1673-1681.
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