Icatibant is a potent bradykinin B2 receptor antagonist peptide for inflammation and allergy research. Buy Icatibant peptide from a reliable peptide supplier to support biomedical studies.
CAT No: 10-101-163
CAS No:130308-48-4
Synonyms/Alias:Icatibant;130308-48-4;Firazyr;icatibanto;HOE 140;UNII-7PG89G35Q7;7PG89G35Q7;Hoechst 140;DTXSID20903963;HOE140;Icatibant [INN];(R)-ARGINYL-(S)-ARGINYL-(S)-PROLYL-(2S,4R)-(4-HYDROXYPROLYL)GLYCYL-(S)-(3-(2-THIENYL)ALANYL)-(S)-SERYL-(R)-((1,2,3,4-TETRAHYDRO-3-ISOQUINOLYL)CARBONYL)-(2S,3AS,7AS)-((HEXAHYDRO-2-INDOLINYL)CARBONYL)-(S)-ARGININE;Icatibant [INN:BAN];icatibantum;icatibant-acetate;D-Arg-(Hyp3,Thi5,D-Tic7,Oic8)BK;JE 049;Icatibant (Standard);Icatibant HOE 140;ICATIBANT [MI];ICATIBANT [VANDF];HOE-140 (Icatibant);ICATIBANT [WHO-DD];ICATIBANT [EMA EPAR];HOE 140 TFA;CHEMBL2028850;SCHEMBL21495177;B06AC02;DTXCID901331902;BDBM50403371;BDBM50406750;HY-17446R;AKOS040741862;AT24149;CS-3381;DB06196;NCGC00390805-02;DA-64221;HY-17446;HOE 140, >=94%;EN300-18166877;Q902379;BRD-K63772874-001-01-4;BRD-K63772874-001-02-2;L-ARGININE, D-ARGINYL-L-ARGINYL-L-PROLYL-TRANS-4-HYDROXY-L-PROLYLGLYCYL-3-(2-THIENYL)-L-ALANYL-L-SERYL-D-1,2,3,4-TETRAHYDRO-3-ISOQUINOLINECARBONYL-L-(2.ALPHA.,3A.BETA.,7A.BETA.)-OCTAHYDRO-1H-INDOLE-2-CARBONYL-;L-Arginine, D-arginyl-L-arginyl-L-prolyl-trans-4-hydroxy-L-prolylglycyl-3-(2-thienyl)-L-alanyl-L-seryl-D-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-L-(2alpha,3abeta,7abeta)-octahydro-1H-indole-2-carbonyl-;
Icatibant is a synthetic decapeptide that functions as a highly selective antagonist of the bradykinin B2 receptor, making it a valuable tool in the study of kinin-kallikrein system biology and bradykinin-mediated signaling pathways. Its peptide structure and receptor specificity have established it as an important research reagent for dissecting the physiological and pathological roles of bradykinin, particularly in the context of inflammation, vascular permeability, and pain transmission. The compound's stability and well-characterized mechanism of action have further contributed to its broad adoption in experimental pharmacology, molecular biology, and peptide-receptor interaction studies.
Receptor Binding Studies: Icatibant is extensively utilized in receptor pharmacology to characterize the binding kinetics and affinity of bradykinin B2 receptors in various cell lines and tissue preparations. By competitively inhibiting bradykinin at its receptor, the compound enables researchers to differentiate between B2 receptor-mediated effects and those arising from other kinin receptors or signaling molecules. This approach is instrumental in mapping receptor distribution, assessing ligand specificity, and elucidating the molecular determinants of receptor-ligand interactions, thereby advancing the understanding of peptide-receptor dynamics in health and disease models.
Signal Transduction Research: As a potent B2 receptor antagonist, icatibant is employed to dissect downstream signaling events triggered by bradykinin activation. Researchers use it to block bradykinin-induced calcium mobilization, nitric oxide production, and other second messenger pathways in endothelial cells, smooth muscle, and neuronal systems. This application is essential for clarifying the contribution of bradykinin signaling to processes such as vasodilation, inflammatory mediator release, and nociceptive transmission, supporting the development of more precise models of cellular response to peptide hormones.
Inflammation and Vascular Permeability Studies: The ability of icatibant to selectively inhibit bradykinin B2 receptors makes it a valuable probe for investigating the role of bradykinin in acute and chronic inflammatory responses. Experimental models frequently incorporate the compound to examine the regulation of vascular permeability, edema formation, and leukocyte recruitment under various inflammatory stimuli. By selectively blocking B2 receptor activity, researchers can delineate the specific contributions of bradykinin to vascular and immune system dynamics, facilitating the identification of potential targets for anti-inflammatory strategies.
Peptide Structure-Activity Relationship (SAR) Analysis: Due to its well-defined sequence and receptor selectivity, icatibant serves as a reference compound in structure-activity relationship studies of bradykinin receptor antagonists. Synthetic chemists and pharmacologists utilize it to benchmark the biological activity of novel peptide analogues, assess modifications in peptide backbone or side chains, and evaluate the impact of structural changes on receptor affinity and antagonist potency. These investigations are crucial for guiding the rational design of next-generation peptide modulators with improved specificity and functional profiles.
In vitro Assay Development: The robust and predictable antagonistic activity of icatibant supports its integration into a variety of in vitro assay platforms designed to screen for bradykinin receptor modulators or to quantify receptor-mediated cellular responses. Its use as a control or reference antagonist enables the standardization of assay conditions, validation of assay sensitivity, and accurate interpretation of experimental outcomes. This application underpins high-throughput screening efforts, mechanistic studies, and the optimization of assay protocols in both academic and industrial research settings.
Icatibant (also called JE049 or HOE140) is a synthetic decapeptide that has a similar structure as bradykinin but contains 5 nonproteinogenic amino acids (D-Arg, L-Hyp, L-Thi, D-Tic, and L-Oic). It is stable and not degraded by bradykinin-cleaving enzymes like carboxypeptidase N (or kininase I) and angiotensin converting enzyme (or kininase II). The study drug was provided by the Jerini AG (Berlin, Germany).
Treatment of acute edema attacks in hereditary angioedema with a bradykinin receptor-2 antagonist (Icatibant)
Icatibant is a selective bradykinin B2 receptor antagonist with, like bradykinin itself, an affinity for the B2 receptor. It does not interact with bradykinin B1 receptors or other peptide receptors. Icatibant reverses increased vascular permeability in C1 esterase inhibitor–knockout mice, inhibits bradykinin-induced vasodilation in humans and, in a phase 1 study, showed dose- and time-dependent inhibition of bradykinin-induced effects in vivo. In a phase 2 study, symptoms improved significantly after open-label treatment with icatibant in 15 patients with hereditary angioedema having acute cutaneous or abdominal attacks.
Icatibant, a New Bradykinin-Receptor Antagonist, in Hereditary Angioedema
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