Deamidated-Eptifibatide

Deamidated-Eptifibatide features a deamidated residue that alters charge distribution and hydrogen-bonding potential. Researchers examine its effects on conformational shifts and receptor-binding characteristics. Applications include impurity characterization, degradation mapping, and structural comparison.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.

CAT No: Z10-101-177

Synonyms/Alias:Deamidated Eptifibatide;618118-95-9;Deamidated Eptifibatide;L-Cysteine, N6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl)-L-lysylglycyl-L-a-aspartyl-L-tryptophyl-L-prolyl-, cyclic (1?6)-disulfide (9CI)

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M.F/Formula
C35H48N10O10S2
M.W/Mr.
833
Sequence
One Letter Code:CXGDWPC
Three Letter Code:deamino-Cys(1)-hArg-Gly-Asp-Trp-Pro-Cys(1)-OH

Deamidated-Eptifibatide is a chemically modified peptide derived from eptifibatide, a well-known cyclic heptapeptide that functions as a potent inhibitor of platelet aggregation. Through the process of deamidation, this analog features subtle structural changes that can significantly influence its biochemical properties, making it a valuable tool for specialized research. Its unique sequence and structural characteristics enable it to interact with integrin receptors, particularly glycoprotein IIb/IIIa, which plays a central role in platelet function and thrombosis. As a result of these properties, Deamidated-Eptifibatide has garnered considerable interest in various fields of biochemical, pharmacological, and molecular research, where understanding the nuances of platelet activation and inhibition is crucial. The peptide's stability and modified binding profile also make it an attractive candidate for in vitro experimentation, mechanistic studies, and the development of novel therapeutic strategies in the laboratory setting.

Platelet Function Studies: In platelet biology research, Deamidated-Eptifibatide serves as a critical probe for dissecting the molecular mechanisms underlying platelet aggregation. By selectively binding to the glycoprotein IIb/IIIa receptor, it enables scientists to evaluate the effects of peptide modifications on receptor affinity and downstream signaling pathways. Researchers utilize it to compare the efficacy and specificity of deamidated versus non-deamidated analogs, thereby gaining insights into the structure-activity relationships that govern integrin-ligand interactions. This comparative approach is particularly valuable for elucidating the fundamental processes that regulate thrombus formation and stability under physiological and pathological conditions.

Drug Discovery and Lead Optimization: In the realm of drug discovery, the deamidated form of eptifibatide is frequently employed as a reference compound or a starting point for designing new glycoprotein IIb/IIIa antagonists. Its altered chemical structure allows medicinal chemists to explore the impact of deamidation on pharmacodynamic and pharmacokinetic profiles, which is essential for optimizing lead compounds. By incorporating this analog into high-throughput screening assays, researchers can identify novel inhibitors with improved selectivity, potency, or metabolic stability. The insights gained from these studies contribute to the rational design of next-generation antiplatelet agents and facilitate the development of safer and more effective therapeutic candidates.

Structural Biology and Protein Engineering: Deamidated-Eptifibatide is an invaluable tool in structural biology, where it aids in elucidating the conformational dynamics of integrin receptors and their ligand-binding domains. Using advanced techniques such as X-ray crystallography, NMR spectroscopy, or cryo-electron microscopy, scientists can investigate how deamidation influences peptide-receptor interactions at the atomic level. These studies not only provide a deeper understanding of the molecular basis of ligand specificity but also inform the engineering of synthetic peptides with tailored properties. As such, it plays a pivotal role in advancing the field of protein engineering and the rational design of biomolecular tools.

Biomarker and Diagnostic Research: In the context of biomarker discovery and diagnostic assay development, deamidated analogs of eptifibatide are utilized to establish sensitive and selective detection methods for platelet activation. By incorporating this peptide into assay platforms, researchers can monitor changes in integrin activity or expression, which are indicative of various hemostatic and thrombotic conditions. The use of deamidated peptides enhances assay specificity and enables the differentiation of closely related receptor subtypes, thereby improving the accuracy and reliability of diagnostic tests. These applications are particularly relevant for basic research laboratories focused on the molecular mechanisms of blood coagulation and platelet function.

Peptide Stability and Metabolism Studies: The deamidated variant of eptifibatide is frequently leveraged in studies aimed at understanding peptide degradation, stability, and metabolic transformation. By comparing the in vitro and in vivo behavior of deamidated versus native peptides, researchers can assess the impact of post-translational modifications on peptide half-life, bioavailability, and susceptibility to enzymatic cleavage. Such investigations are critical for optimizing peptide-based drug candidates and for designing analogs with enhanced resistance to metabolic breakdown. The knowledge generated from these studies informs the development of robust peptide therapeutics and supports the broader field of peptide chemistry research. Through its multifaceted applications, Deamidated-Eptifibatide continues to be an essential tool for advancing scientific knowledge in platelet biology, drug discovery, structural biology, diagnostics, and peptide engineering.

InChI
InChI=1S/C35H48N10O10S2/c36-35(37)38-11-4-3-8-22-30(50)40-17-28(47)42-23(15-29(48)49)31(51)43-24(14-19-16-39-21-7-2-1-6-20(19)21)33(53)45-12-5-9-26(45)32(52)44-25(34(54)55)18-57-56-13-10-27(46)41-22/h1-2,6-7,16,22-26,39H,3-5,8-15,17-18H2,(H,40,50)(H,41,46)(H,42,47)(H,43,51)(H,44,52)(H,48,49)(H,54,55)(H4,36,37,38)/t22-,23-,24-,25-,26-/m0/s1
InChI Key
FKUGYENQIXKJRH-LROMGURASA-N

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