SLIGKV-NH2

Non Antibodies

Protease-activated receptor-2 (PAR2)

The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture.

614.77 Da

A Potent Agonist of PAR2, Derived from PAR2 Auto-Ligand Sequence

Centrifuge the vial (10, 000 × g for 5 minutes) before adding solvent to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Gently tap, tilt, and roll the vial to aid dissolution. Avoid vigorous vortexing; light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity.

7, 4

Val⁶ - C-terminal amidation

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.

no

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.