Protease-Activated Receptor-2, amide 

Protease-Activated Receptor-2, amide (SLIGKV-NH₂) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.

The PAR2-activating peptides used are: SLIGKV-OH, SLIGRL-OH, SLIGKV-NH₂, SLIGRL-NH₂. The synthetic agonist peptides mimicking the tethered ligand of PAR2, Ser-Leu-Ile-Gly-Lys-Val (SLIGKV-OH), Ser-Leu-Ile-Gly-Arg-Leu (SLIGRL-OH) and their amidated forms Ser-Leu-Ile-Gly-Lys-Val-amide (SLIGKV-NH₂) Ser-Leu-Ile-Gly-Arg-Leu-amide (SLIGRL-NH₂) have also been demonstrated being able to activate the receptor without enzymatic cleavage, therefore, have been utilised as biological tools to examine physiological functions of PAR2. Protease-Activated Receptor-2, amide is one of a four family subgroup of G-protein-coupled receptors (GPCRs), called PARs. Protease-activated receptors are distinguished from other GPCRs through their unique proteolytic mechanism of activation. For PAR2, activating proteases, such as trypsin, tryptase and coagulation factors VIIa and Xa, cleave a specific extracellular amino-terminal domain of the receptor to reveal a "tethered ligand", SLIGKV- and SLIGRL- for human and mouse/rat PAR2, respectively, which subsequently interacts with the activation domain of the receptor, initiating intracellular signaling pathways^[1]. The protease-activated receptor-2 (PAR2) has been implicated in the pathogenesis of several inflammatory and autoimmune disorders, and is expressed in a wide variety of human tissues and cells. PAR2 belongs to a family of seven transmembrane domain receptor proteins that are activated by proteolysis. Enzymatic digestion exposes an N-terminus ligand sequence that binds intramolecularly to the activation site on the extracellular loop II, initiating a G-protein-mediated cell-signalling cascade and nuclear factor-kappa B (NF-κB)-regulated gene transcription^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

614.78

C₂₈H₅₄N₈O₇

190383-13-2

Solid

White to off-white

Ser-Leu-Ile-Gly-Lys-Val-NH2

SLIGKV-NH2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Kanke T, et al. Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2. Br J Pharmacol. 2005 May;145(2):255-63.  [Content Brief]

  [2]. Ramelli G, et al. Protease-activated receptor 2 signalling promotes dendritic cell antigen transport and T-cellactivation in vivo. Immunology. 2010 Jan;129(1):20-7.  [Content Brief]