PROTEASE-ACTIVATED RECEPTOR-2 AGONIST, AMIDE
H-SER-LEU-ILE-GLY-LYS-VAL-NH2
CAS: 190383-13-2
Molecular Formula: C28H54N8O7
PROTEASE-ACTIVATED RECEPTOR-2 AGONIST, AMIDE - Names and Identifiers
PROTEASE-ACTIVATED RECEPTOR-2 AGONIST, AMIDE - Physico-chemical Properties
| Molecular Formula | C28H54N8O7 |
| Molar Mass | 614.78 |
| Appearance | solid |
| Storage Condition | -20°C |
| In vitro study | The PAR2-activating peptides used are: SLIGKV-OH, SLIGRL-OH, SLIGKV-NH 2 , SLIGRL-NH 2 . 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-NH 2 ) Ser-Leu-Ile-Gly-Arg-Leu-amide (SLIGRL-NH 2 ) 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. 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. |
PROTEASE-ACTIVATED RECEPTOR-2 AGONIST, AMIDE - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
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