Icatibant Acetate is the acetate salt form of icatibant, an antagonist of the human bradykinin B2 receptor (B2R).
CAT No: HB00111
CAS No:138614-30-9
Synonyms/Alias:Icatibant acetate;Firazyr;Hoe-140;138614-30-9;Icatibant (acetate);Icatibant acetate [USAN];UNII-325O8467XK;Hoechst 140;325O8467XK;HOE 140;HOE140;(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 acetate (salt);ICATIBANT ACETATE (MART.);ICATIBANT ACETATE [MART.];L-ARGININE, D-ARGINYL-L-ARGINYL-L-PROLYL-(4R)-4-HYDROXY-L-PROLYLGLYCYL-3-(2-THIENYL)-L-ALANYL-L-SERYL-(3R)-1,2,3,4-TETRAHYDRO-3-ISOQUINOLINECARBONYL-(2S,3AS,7AS)-OCTAHYDRO-1H-INDOLE-2-CARBONYL-, ACETATE;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-, acetate (salt);Hoechst-140;Icatibant acetate?;(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 acetate (salt);JE-049;SAJAZIR;JE049;ICATIBANT ACETATE [MI];ICATIBANT ACETATE [JAN];CHEMBL2028852;ICATIBANT ACETATE [WHO-DD];138614-30-9 , xAcetate;AKOS040745043;ICATIBANT ACETATE [ORANGE BOOK];DA-54232;MS-32135;HY-108896;CS-0031296;Q27256146;(R)-arginyl-(S)-arginyl-()-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 acetate;D-Arginyl-L-arginyl-L-prolyl-(R)-4-hydroxy-L-prolylglycyl-3-(thiophen-2-yl)-L-alanyl-L-seryl-(R)-((1,2,3,4-tetrahydroisoquinolin-3-yl)carbonyl)-(2S,3aS,7aS)-((hexahydroindolin-2-yl)carbonyl)-L-arginine triacetate;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-, ACETATE (SALT);
Icatibant Acetate is a synthetic decapeptide that functions as a potent and selective antagonist of the bradykinin B2 receptor. Structurally derived to mimic natural peptide substrates while resisting enzymatic degradation, it plays a significant role in the study of inflammatory pathways, vascular permeability, and pain signaling. Its unique biochemical properties and receptor specificity make it an indispensable tool for researchers investigating the molecular mechanisms of bradykinin-mediated responses, as well as for those developing and validating new pharmacological agents targeting the kallikrein-kinin system.
Receptor Pharmacology: Icatibant Acetate is widely utilized in receptor binding and functional assays to elucidate the role of bradykinin B2 receptors in various physiological and pathological contexts. By competitively inhibiting bradykinin binding, it allows for precise mapping of receptor-mediated signaling cascades in diverse cell types and tissue preparations. This enables researchers to dissect downstream effects such as calcium mobilization, nitric oxide production, and prostaglandin release, providing critical insights into inflammatory and nociceptive processes.
Inflammatory Pathway Research: Due to its ability to selectively block bradykinin-induced responses, this peptide antagonist is instrumental in studying the molecular basis of inflammation and vascular leakage. Experimental models employing Icatibant Acetate facilitate the characterization of kinin-mediated edema, leukocyte migration, and cytokine release. Such studies are essential for understanding the contribution of the kallikrein-kinin system to acute and chronic inflammatory diseases, supporting the identification of novel anti-inflammatory targets.
Peptide Drug Development: The structural features and receptor selectivity of Icatibant Acetate make it a valuable reference compound in the development and optimization of new peptide-based B2 receptor antagonists. Its use in comparative pharmacological profiling and structure-activity relationship (SAR) studies helps guide the rational design of next-generation molecules with improved potency, selectivity, and metabolic stability. Synthetic chemists and pharmacologists benefit from its well-characterized activity profile when benchmarking candidate compounds.
Signal Transduction Studies: In cellular and ex vivo systems, Icatibant Acetate is employed to delineate the signaling pathways activated by bradykinin B2 receptor stimulation. By selectively inhibiting receptor function, it enables detailed investigation of G protein-coupled receptor (GPCR) signaling, second messenger dynamics, and cross-talk with other receptor systems. This is particularly valuable in neurobiology, cardiovascular research, and studies of pain perception, where bradykinin signaling plays a pivotal role.
Analytical and Bioassay Development: Icatibant Acetate serves as a standard or control in the development and validation of bioanalytical assays targeting bradykinin B2 receptor activity. Its defined pharmacological properties allow for the calibration and quality control of high-throughput screening platforms, receptor binding assays, and cell-based functional assays. This supports the generation of reproducible, quantitative data necessary for both basic research and the preclinical evaluation of new therapeutic candidates targeting the kinin system.
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