Overview
Alternative Name PAR2 agonist, PAR2AP
Lyophilized Powder yes
Origin Synthetic peptide
MW: 614.78 Da
Purity: >98% (HPLC)
Effective concentration 10-250 μM.
Sequence SLIGKV.
Modifications Val6 - C-terminal amidation .
Molecular formula C28H54N8O7.
CAS No.: 190383-13-2
Activity SLIGKV-NH2 is a selective agonist of the Protease-activated receptor-2 (PAR2)1. The peptide is composed of the neo-N-terminal 6 amino acids of human PAR2, after receptor activation by protease cleavage1.
References-Activity
- Ossovskaya V. S. and Bunnett N. W. (2004) Physiol. Rev. 84, 579.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to one week at 4°C or three months at -20°C.
Our bioassay
Alomone Labs SLIGKV-NH2 induces MAPK activation in MDA-231 cells via PAR2 activation.MDA-231 cells were stimulated with 10, 50 and 250 µM SLIGKV-NH2 (#GPS-100) for 15 min. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho-ERK1/2.
References - Scientific background
- Ossovskaya VS. et al. (2004) Physiol Rev. 84, 579.
- Rattenholl A. et al. (2008) Drug News Perspect. 21, 369.
- Boitano S. et al. (2011) J. Med. Chem. 54, 1308.
- Barry GD. et al. (2006) Curr. Med. Chem. 13, 243.
- Steinhoff M. et al. (2005) Endocr. Rev. 26, 1.
- Cottrell GS. et al. (2003) Biochem. Soc. Trans. 31, 1191.
- Ramachandran R. et al. (2008) Br. J. Pharmacol. 153, S263.
Scientific background Protease-activated receptors (PARs) 1-4 belong to the superfamily of G-protein-coupled receptors (GPCRs) that are self-activated by a tethered sequence exposed by proteolysis of an extracellular domain1. PARs are activated by proteolysis in response to endogenous and exogenous proteases and can contribute to both cellular homeostasis and pathology1-2. In the case of PAR2, the exposed human peptide SLIGVK-NH2 remains tethered on the receptor and activates a primary binding site located on second loop of the receptor1. As an obvious consequence of its activation mechanism, PAR2 is associated with pathologies with a strong protease release. The involvement of PAR2 in inflammatory diseases such as arthritis, lung inflammation (asthma), inflammatory bowel disease, sepsis, and pain disorders4-6 makes PAR2 an attractive target for drug intervention3. The extracellular N-terminus of PAR2 (46 residues long) contains a putative trypsin cleavage site R34 and S351, followed by LIGKV. The human-derived SLIGKV-NH2 is a small peptide that mimics the ligand binding properties of the tethered ligand exposed by proteolysis of the N-terminus from the natural receptor7 and hence, a significant tool used to study PAR2.
Peptide Content: 100%
Lyophilized Powder
SLIGKV-NH2 (#GPS-100) is a highly pure, synthetic, and biologically active peptide.
For research purposes only, not for human use
Last Update: 07/05/2024
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