Deltibant is a peptide derivative containing aromatic, aliphatic, and charged residues arranged to modulate binding surfaces. Its sequence supports studies of structural rigidity and solvent-peptide interface dynamics. Researchers apply it in mapping recognition motifs and probing peptide stability. Its defined architecture encourages thorough biophysical evaluation.
CAT No: R1934
CAS No:140661-97-8
Synonyms/Alias:Deltibant;140661-97-8;Deltibant [USAN:INN];UNII-6151J4V7VX;6151J4V7VX;DELTIBANT [INN];DELTIBANT [MI];DELTIBANT [USAN];DELTIBANT [WHO-DD];D-Arginyl-L-arginyl-L-prolyl-trans-4-hydroxy-L-prolyl-S-(1-(6-(3-mercapto-2,5-dioxo-1-pyrrolidinyl)hexyl)-2,5-dioxo-3-pyrrolidinyl)-L-cysteinyl-L-phenylalanyl-L-seryl-D-phenylalanyl-L-leucyl-L-arginine (5-5')-sulfide with D-arginyl-L-arginyl-L-prolyl-trans-4-hydroxy-L-prolyl-L-cysteinyl-L-phenylalanyl-L-seryl-D-phenylalanyl-L-leucyl-L-arginine;D-Arginyl-L-arginyl-L-prolyl-trans-4-hydroxy-L-prolylgylcyl-L-phenylalanyl-L-cysteinyl-D-phenylalanyl-L-leucyl-L-arginine, 7,7'-bis(sulfide) with (2R,2'S)-N,N'-hexamethylenebis(2-mercaptosuccinimide);L-Arginine, D-arginyl-L-arginyl-L-prolyl-trans-4-hydroxy-L-prolyl-S-(1-(6-(3-mercapto-2,5-dioxo-1-pyrrolidinyl)hexyl)-2,5-dioxo-3-pyrrolidinyl)-L-cysteinyl-L-phenylalanyl-L-seryl-D-phenylalanyl-L-leucyl-, (5-5')-sulfide with D-arginyl-L-arginyl-L-prolyl-trans-4-hydroxy-L-prolyl-L-cysteinyl-L-phenylalanyl-L-seryl-D-phenylalanyl-L-leucyl-L-arginine;deltibantum;CP 0127;SCHEMBL1230580;CHEMBL2103953;
Chemical Name:(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2S)-2-[[2-[[(2S,4R)-1-[(2S)-1-[(2S)-2-[[(2R)-2-amino-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]-4-hydroxypyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-[(3S)-1-[6-[(3R)-3-[(2R)-2-[[(2S)-2-[[2-[[(2S,4R)-1-[(2S)-1-[(2S)-2-[[(2R)-2-amino-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]-4-hydroxypyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-[[(2R)-1-[[(2S)-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]hexyl]-2,5-dioxopyrrolidin-3-yl]sulfanylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoic acid
Deltibant is a synthetic peptide compound recognized for its role as a selective bradykinin B2 receptor antagonist. As a member of the peptide inhibitor class, it is designed to specifically block the action of bradykinin, a key mediator involved in various physiological and pathological processes such as inflammatory responses, vascular permeability, and pain signaling. Due to its high specificity and well-characterized mechanism of action, deltibant has become a valuable tool in biochemical and pharmacological research focused on elucidating the functional significance of bradykinin pathways. Its application extends across multiple research domains, offering insights into complex signaling cascades and supporting the development of new investigative models for inflammation and vascular biology.
Inflammatory pathway research: Deltibant is extensively used in studies investigating the molecular mechanisms underlying inflammation. By selectively inhibiting bradykinin B2 receptors, it allows researchers to dissect the specific contributions of bradykinin signaling to inflammatory cascades in both in vitro and in vivo models. This enables the identification of downstream effectors and the mapping of cytokine networks influenced by bradykinin, supporting the development of targeted anti-inflammatory strategies and the validation of novel biomarkers associated with inflammatory states.
Vascular permeability studies: The peptide's ability to modulate bradykinin-induced responses makes it a critical reagent in research focused on vascular permeability and endothelial function. It is employed to quantify the role of bradykinin in promoting vascular leakage and edema formation, thereby facilitating the assessment of endothelial barrier integrity under experimental conditions. Such studies provide a clearer understanding of the molecular events that govern tissue fluid balance and are instrumental in developing in vitro models of barrier dysfunction.
Pain signaling investigations: Deltibant serves as a powerful tool in the exploration of nociceptive pathways, particularly those mediated by bradykinin. By antagonizing B2 receptors, it helps delineate the specific contribution of bradykinin to pain perception and hypersensitivity. Researchers utilize the compound to differentiate between receptor-mediated and non-receptor-mediated pain mechanisms, advancing the fundamental understanding of pain transduction and supporting the refinement of experimental pain models.
Receptor binding and pharmacological profiling: As a highly selective peptide antagonist, deltibant is frequently used in receptor binding assays and pharmacological characterization studies. It enables precise quantification of bradykinin B2 receptor density, affinity, and functional responsiveness in various cell types and tissue preparations. Such profiling is essential for validating receptor-specific effects, screening for novel modulators, and establishing reliable reference standards for comparative pharmacological analyses.
Peptide structure-activity relationship (SAR) studies: The well-defined sequence and receptor selectivity of deltibant make it an ideal model compound for peptide SAR investigations. Researchers employ it to evaluate the impact of structural modifications on receptor binding, antagonist potency, and metabolic stability. Insights gained from these studies inform rational peptide design and contribute to the broader understanding of peptide-receptor interactions, facilitating the development of next-generation peptide tools and inhibitors for research applications.
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