Description
SLIGRL-NH2 is a recombinant peptide that activates PAR2 (EC50 = ~5 µM), without requiring receptor cleavage.1,2 This peptide does not activate PAR1. Through its effects on PAR2, SLIGRL-NH2 stimulates gastric and intestinal smooth muscle contraction and induces thermal hyperalgesia in mice.3,4 SLIGRL-NH2 is used to explore signaling through PAR2 in cells and in animals.5,6WARNING This product is not for human or veterinary use.
References
[1] S NYSTEDT. Molecular cloning of a potential proteinase activated receptor.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1994, 91 20: 9208-9212. DOI: 10.1073/pnas.91.20.9208
[2] S NYSTEDT. The mouse proteinase-activated receptor-2 cDNA and gene. Molecular cloning and functional expression.[J]. The Journal of Biological Chemistry, 1995, 270 11: 5950-5955. DOI: 10.1074/jbc.270.11.5950
[3] ATSUFUMI KAWABATA. In vivo evidence that protease-activated receptors 1 and 2 modulate gastrointestinal transit in the mouse[J]. British Journal of Pharmacology, 2009, 133 8: 1213-1218. DOI: 10.1038/sj.bjp.0704211
[4] QIN LIU. The Distinct Roles of Two GPCRs, MrgprC11 and PAR2, in Itch and Hyperalgesia[J]. Science Signaling, 2011, 4 181. DOI: 10.1126/scisignal.2001925
[5] WIMOLPAK SRIWAI. Distinctive G Protein-Dependent Signaling by Protease-Activated Receptor 2 (PAR2) in Smooth Muscle: Feedback Inhibition of RhoA by cAMP-Independent PKA.[J]. PLoS ONE, 2013: e66743. DOI: 10.1371/journal.pone.0066743
[6] SARINA B ELMARIAH Ethan A L Vemuri B Reddy. Cathepsin S signals via PAR2 and generates a novel tethered ligand receptor agonist.[J]. PLoS ONE, 2014: e99702. DOI: 10.1371/journal.pone.0099702
