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, also known as a selective bradykinin B2 receptor antagonist, is a synthetic decapeptide that has garnered significant attention in biochemical and pharmacological research. Its unique structure enables it to effectively block the action of bradykinin, a peptide involved in various physiological and pathological processes such as inflammation, vascular permeability, and pain signaling. Icatibant's stability and specificity make it a valuable tool for investigating the intricate pathways mediated by bradykinin, allowing researchers to dissect the roles of this peptide in diverse biological systems. The compound's ability to selectively antagonize the B2 receptor without affecting other pathways ensures precise modulation in experimental models, making it indispensable for studies aiming to elucidate the molecular mechanisms underlying bradykinin-mediated responses.
Inflammation Research: Icatibant is widely used in the study of inflammatory pathways, particularly those involving the kallikrein-kinin system. By inhibiting the interaction between bradykinin and its B2 receptor, researchers can investigate the contribution of this signaling axis to acute and chronic inflammation. This approach is instrumental in exploring the molecular underpinnings of tissue edema, leukocyte infiltration, and cytokine production in various experimental models. The insights gained from such studies are crucial for identifying novel therapeutic targets for inflammatory diseases and for understanding the complex interplay between different mediators involved in the inflammatory response.
Pain Mechanism Studies: The compound serves as an essential reagent in pain research, especially in models of nociceptive and neuropathic pain. By blocking bradykinin-induced activation of sensory neurons, Icatibant allows scientists to delineate the specific pathways through which bradykinin contributes to pain perception and hypersensitivity. This targeted approach aids in distinguishing the roles of different pain mediators and in evaluating the efficacy of potential analgesic compounds. Additionally, the use of this peptide antagonist facilitates the identification of downstream signaling events that are critical for the development and maintenance of pain states.
Vascular Permeability Investigations: Researchers utilize Icatibant to study the regulation of vascular permeability and the mechanisms leading to plasma extravasation. Bradykinin is a key mediator of increased vascular permeability, and its inhibition provides valuable data on the processes governing endothelial barrier function. By employing this antagonist in in vitro and in vivo models, scientists can assess the impact of bradykinin signaling on the integrity of blood vessels, the formation of edema, and the migration of immune cells. These studies are fundamental for advancing the understanding of vascular biology and for identifying strategies to modulate pathological fluid leakage.
Allergy and Hypersensitivity Models: The compound is also instrumental in allergy research, where it is used to investigate the role of bradykinin in hypersensitivity reactions. By selectively blocking the B2 receptor, Icatibant helps clarify the contribution of bradykinin to symptoms such as swelling, redness, and itching in experimental models of allergic responses. This application is particularly valuable for differentiating the effects of various mediators released during allergic reactions and for exploring potential interventions aimed at mitigating hypersensitivity symptoms.
Experimental Pharmacology: In pharmacological research, Icatibant is employed as a reference antagonist to evaluate the specificity and efficacy of novel compounds targeting the bradykinin pathway. Its well-characterized mechanism of action and robust antagonist properties make it an ideal control in assays designed to screen for new B2 receptor modulators. By comparing the effects of candidate molecules with those of Icatibant, researchers can accurately assess the pharmacodynamic properties and receptor selectivity of investigational agents. This application supports the rational design and optimization of new molecules for research and therapeutic purposes, reinforcing the importance of Icatibant in experimental pharmacology and drug discovery.
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
1. Emerging applications of nanotechnology for diagnosis and therapy of disease: a review
4. High fat diet and GLP-1 drugs induce pancreatic injury in mice
5. Autoinhibition and phosphorylation-induced activation of phospholipase C-γ isozymes
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More