2-Furoyl-LIGRLO-amide is a potent, selective protease-activated receptor 2 (PAR2) agonist where PAR-2 activation is associated with increases in cAMP and intracellular Ca(2+). Immunoblot analysis revealed, increases in phosphorylation of epidermal growth factor (EGF) receptor (EGFR) tyrosine kinase, Src, Pyk2, cRaf, and ERK1/2 in response to PAR-2 activation.
CAT No: R1835
CAS No:729589-58-6
Synonyms/Alias:2-furoyl-LIGRLO-amide;729589-58-6;2-(2-Furoyl)-leu-ile-gly-arg-leu-orn-nh2;CHEMBL509819;N-[(2S)-1-[[(2S,3S)-1-[[2-[[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-1-[[(2S)-1,5-diamino-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]furan-2-carboxamide;fur-2-oyl-Leu-Ile-Gly-Arg-Leu-Orn-NH2;GLXC-25026;HY-P1314;BDBM50412718;AKOS024457384;MS-31409;PD019049;CS-0029361;G13493;
2-Furoyl-LIGRLO-amide is a synthetic peptide agonist recognized for its specificity and potency in modulating protease-activated receptor-2 (PAR2) signaling pathways. Structurally, it incorporates a 2-furoyl moiety at the N-terminus of the hexapeptide LIGRLO-amide, which enhances its receptor affinity and stability compared to native PAR2-activating peptides. The compound is widely utilized in research settings to dissect the molecular mechanisms underlying PAR2-mediated cellular responses, providing a valuable biochemical tool for the study of signal transduction, inflammation, and related physiological processes. Its defined sequence and robust activity profile make it an indispensable reagent in the field of peptide-based receptor biology.
Receptor activation studies: 2-Furoyl-LIGRLO-amide serves as a highly selective agonist for PAR2, enabling precise interrogation of receptor activation mechanisms in diverse cellular models. Researchers employ this peptide to stimulate PAR2 in vitro, facilitating the assessment of downstream signaling events such as calcium mobilization, MAPK pathway activation, and gene expression changes. Its use allows for controlled and reproducible activation of PAR2, supporting the elucidation of receptor function in both native and engineered cell systems.
Inflammatory pathway research: The compound is instrumental in exploring the role of PAR2 in inflammation and immune modulation. By activating PAR2 on target cells such as endothelial cells, epithelial cells, or immune cell subsets, the peptide enables detailed studies of cytokine release, barrier function, and leukocyte recruitment. Its application aids in clarifying the contribution of PAR2 signaling to inflammatory cascades, tissue injury responses, and chronic disease models, thereby advancing understanding of fundamental immunological processes.
Pharmacological profiling: 2-Furoyl-LIGRLO-amide is frequently employed in pharmacological assays to benchmark the efficacy and selectivity of candidate PAR2 modulators. Its well-characterized agonistic activity provides a reliable standard for evaluating antagonist potency, receptor desensitization, or biased signaling phenomena. Use in dose-response experiments and competitive binding assays supports the development of novel therapeutic strategies targeting PAR2 and related G protein-coupled receptors.
Peptide structure-activity relationship (SAR) studies: The defined sequence and N-terminal modification of this peptide make it a valuable reference compound in SAR investigations. Researchers use it to compare the biological activity of structural analogs, analyze the impact of amino acid substitutions, and optimize peptide design for enhanced receptor selectivity or stability. Such studies contribute to a deeper understanding of the molecular determinants governing peptide-receptor interactions and inform the rational design of next-generation receptor agonists.
Cellular signaling pathway elucidation: The ability of 2-Furoyl-LIGRLO-amide to trigger discrete signaling cascades downstream of PAR2 activation makes it a preferred tool for dissecting complex cellular networks. Researchers leverage its activity to map intracellular signaling nodes, study cross-talk with other receptor systems, and investigate temporal dynamics of signal propagation. These applications are critical for unraveling the multifaceted roles of PAR2 in cell physiology and pathophysiology, enabling targeted exploration of receptor-driven processes in health and disease models.
2. Autoinhibition and phosphorylation-induced activation of phospholipase C-γ isozymes
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