2-Furoyl-LIGRLO-amide

Product Name:2-Furoyl-LIGRLO-amide

CAS No:729589-58-6

Purity:95%

Molar Mass:777.96

Chemical Formula:C36H63N11O8

Storage:Store at -20 degrees Celsius

Sequence:LIGRLX

Target:PAR2

Application:

2-Furoyl-LIGRLO-amide is a potent and selective agonist for Protease-Activated Receptor 2 (PAR2), a G protein-coupled receptor involved in a range of physiological and pathological processes. This peptide is widely used in research to explore the signaling mechanisms of PAR2, which plays critical roles in inflammation, pain, and tissue repair. Activation of PAR2 by 2-Furoyl-LIGRLO-amide can help to elucidate its involvement in diseases such as asthma, arthritis, cancer, and inflammatory bowel disease. It is a valuable tool in the development of therapeutic agents targeting PAR2-related pathways, offering insights into new treatment approaches for inflammatory and pain-related disorders.

Current Research:

2-Furoyl-LIGRLO-amide is a synthetic peptide agonist selective for the protease-activated receptor 2 (PAR2). PAR2, a member of the G protein-coupled receptor (GPCR) family, is activated by proteolytic cleavage, releasing a tethered ligand that binds intramolecularly to the receptor. 2-Furoyl-LIGRLO-amide mimics this activation mechanism, allowing researchers to study PAR2-related pathways without the need for proteolytic activity.

Chemical Properties
The 2-furoyl group enhances the peptide’s stability and receptor binding affinity. Its sequence, LIGRLO-amide, represents a key activating motif for PAR2, and the terminal amide further stabilizes the peptide.

Biological Activity

PAR2 Activation: 2-Furoyl-LIGRLO-amide selectively activates PAR2, eliciting responses such as intracellular calcium mobilization and activation of signaling cascades, including ERK1/2 phosphorylation.
Inflammation and Pain Modulation: PAR2 is involved in inflammatory and pain pathways, making this peptide a valuable tool for studying mechanisms underlying inflammatory diseases and nociception.
Vascular and Gastrointestinal Functions: PAR2 plays roles in vascular tone regulation and gut motility, and this peptide aids in elucidating these physiological processes.
Applications in Research

Inflammation Studies: By activating PAR2, 2-Furoyl-LIGRLO-amide helps researchers investigate the receptor’s role in inflammatory diseases such as arthritis, asthma, and colitis.
Pain Research: It is used to model PAR2-mediated hyperalgesia and explore therapeutic interventions for chronic pain conditions.
Signal Transduction: The peptide is critical for dissecting PAR2 signaling pathways and their contributions to disease pathophysiology.
Advantages
Compared to natural protease activators, 2-Furoyl-LIGRLO-amide offers precise and controlled activation of PAR2, avoiding off-target effects associated with protease activity.

Conclusion
2-Furoyl-LIGRLO-amide is a highly selective and stable PAR2 agonist. Its applications in studying inflammation, pain, and signal transduction pathways make it an indispensable tool in pharmacological and physiological research.

Reference:

Hollenberg, M. D., Renaux, B., Hyun, E., Houle, S., Vergnolle, N., Saifeddine, M., & Ramachandran, R. (2008). Derivatized 2-furoyl-LIGRLO-amide, a versatile and selective probe for proteinase-activated receptor 2: binding and visualization. Journal of Pharmacology and Experimental Therapeutics, 326(2), 453-462.