Dalazatide, an avant-garde peptide-driven medicinal compound, finds its profound utility within the expansive realm of the biomedical industry, effectively tackling the debilitating complexities of autoimmunity afflicting individuals, specifically those burdened by rheumatoid arthritis and multiple sclerosis. Its therapeutic prowess resides within the astute manipulation of purposefully obstructing designated potassium channels, thus suppressing immune cell hyperactivity by alleviating inflammation.
CAT No: R1979
CAS No:1081110-69-1
Synonyms/Alias:Dalazatide;Dalazatide [INN];1081110-69-1;SHK-186;UNII-6U0259J807;6U0259J807;o-PHOSPHONO-L-Tyrosyl-2-(2-(2-aminoethoxy)ethoxy)acetyl(potassium channel toxin kappa-stichotoxin-shela stoichactis helianthus (caribbean sea anemone)) peptidamide;DA-72541;
Chemical Name:2-[(1R,2aS,4S,7S,10S,13S,19S,22S,25S,28S,31R,36R,39S,48S,51S,54S,57R,60S,63S,66S,69S,72S,75S,78S,81S,84S,87S,90R,93S,96S,99S)-31-[[(2S)-2-[[(2R)-2-[acetyl-[(2S)-2-amino-3-(4-phosphonooxyphenyl)propanoyl]amino]-2-[2-(2-aminoethoxy)ethoxy]-5-carbamimidamidopentanoyl]amino]-3-hydroxypropanoyl]amino]-10,51,75,87-tetrakis(4-aminobutyl)-93-(3-amino-3-oxopropyl)-60,96-dibenzyl-19,28-bis[(2S)-butan-2-yl]-4,54,69-tris(3-carbamimidamidopropyl)-36-carbamoyl-2a,22,39,48-tetrakis[(1R)-1-hydroxyethyl]-7,63,81-tris(hydroxymethyl)-72-[(4-hydroxyphenyl)methyl]-84-(1H-imidazol-4-ylmethyl)-99-methyl-66-(2-methylpropyl)-78-(2-methylsulfanylethyl)-1a,3,4a,6,9,12,18,21,24,27,30,38,41,44,47,50,53,56,59,62,65,68,71,74,77,80,83,86,89,92,95,98-dotriacontaoxo-6a,7a,10a,11a,33,34-hexathia-a,2,3a,5,8,11,17,20,23,26,29,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85,88,91,94,97-dotriacontazatetracyclo[55.47.4.445,90.013,17]dodecahectan-25-yl]acetic acid
Dalazatide is a synthetic peptide compound that functions as a selective inhibitor of the Kv1.3 potassium channel, a critical regulator of membrane potential and cellular activation in various immune cell types. As a member of the peptide toxin family derived from sea anemone venom, Dalazatide exhibits high affinity and specificity for Kv1.3 channels, making it a valuable tool for dissecting ion channel pharmacology and understanding the molecular mechanisms underlying immune cell signaling. Its unique biochemical profile has positioned it as a prominent research reagent in the fields of immunology, electrophysiology, and peptide-based drug discovery, offering significant utility for scientists exploring the roles of ion channels in health and disease.
Ion channel research: Dalazatide is widely employed in studies focused on the functional characterization of voltage-gated potassium channels, particularly Kv1.3. By selectively blocking this channel, researchers can investigate the biophysical properties, gating mechanisms, and pharmacological modulation of Kv1.3 in various cellular contexts. The compound's high specificity allows for the discrimination of Kv1.3 activity from related potassium channels, facilitating detailed analyses of channelopathies and contributing to the development of novel ion channel modulators.
Immunology studies: The peptide's ability to selectively inhibit Kv1.3 channels in T lymphocytes has made it an indispensable tool in immunological research. Kv1.3 plays a pivotal role in the activation and proliferation of effector memory T cells, and Dalazatide enables researchers to dissect the downstream signaling pathways regulated by potassium flux in these immune subsets. Its use supports investigations into the molecular basis of immune cell activation, calcium signaling, and cytokine production, providing insights into the pathophysiology of immune-mediated conditions.
Electrophysiological assays: Dalazatide is frequently utilized in patch-clamp and other electrophysiological techniques to study the dynamics of potassium channel currents in both native and recombinant systems. Its high potency and selectivity allow for precise manipulation of Kv1.3-mediated currents, enabling the quantification of channel kinetics, conductance properties, and pharmacological responses. This application is essential for validating Kv1.3 as a target in cellular models and for screening new channel modulators in drug discovery pipelines.
Peptide engineering and structure-activity relationship (SAR) studies: As a synthetic peptide derived from a natural toxin, Dalazatide serves as a reference molecule for peptide engineering projects aimed at improving channel selectivity, stability, or pharmacokinetic properties. Researchers leverage its well-characterized structure to design and synthesize analogs, map critical binding residues, and evaluate the impact of amino acid substitutions on biological activity. Such studies advance the development of next-generation peptide modulators with optimized properties for research and potential translational applications.
Autoimmune disease modeling: While not intended for clinical or therapeutic use, Dalazatide is frequently used in preclinical models to probe the contribution of Kv1.3 channels to immune cell function in autoimmune settings. By selectively inhibiting these channels, scientists can assess the impact on T cell-mediated responses, tissue infiltration, and inflammatory signaling. These experimental models help clarify the mechanistic underpinnings of autoimmune pathogenesis and support the identification of novel targets for immunomodulatory interventions in a research context.
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