PAR-2 agonist SLIGRL-amide

Description

Representing the activating sequence of the “tethered ligand” of protease cleaved mouse PAR-2

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Catalogue number crb1000216
Sequence (one letter code) SLIGRL-amide
Sequence (three letter code) H-Ser-Leu-Ile-Gly-Arg-Leu-NH2
Aliases PAR-2 agonist
Purity >95%
Storage -20°C
Molecular Weight 656.4
References

Zhang, H., Zeng, X. and He, S. (2014). Evaluation on Potential Contributions of Protease Activated Receptors Related Mediators in Allergic Inflammation. Mediators Inflamm, 2014, 1-20. PMID: 24876677

Moffatt, J. D., Jeffrey, K. L. and Cocks, T. M. (2002). Protease-Activated Receptor-2 Activating Peptide SLIGRL Inhibits Bacterial Lipopolysaccharide-Induced Recruitment of Polymorphonuclear Leukocytes into the Airways of Mice. Am J. Respir Cell Mol Biol, 2002, 26: 680–684

Protease activated receptors (PARs) are a distinctive four-member family of seven transmembrane G protein-coupled receptors (GPCRs) widely expressed in inflammatory cells. PARs are cleaved by certain serine proteases to expose a tethered ligand domain, this ligand domain then binds to and activates the receptors to initiate multiple signalling cascades. These PAR-activating proteases therefore represent PAR agonists. This PAR-2 agonist peptide mimics the sequence of the “tethered ligand” and is therefore capable of activating the receptor independently of N-terminal proteolysis.


SLIGRL-NH2 inhibits the development of airway eosinophilia, hyper-responsiveness and displays bronchodilator activity in allergic mice and also facilitates gastrointestinal transit in mice in vivo.


PAR activation has been linked to inflammation, therefore compounds that mimic or interfere with the PAR-activating processes are attractive therapeutic candidates.

PAR-2 agonist

Cat No. Pack Size Price Qty

crb1000216h

0.5mg

$112.50

crb1000216j

1mg

$150.00