Name | sligrl-nh2 |
---|---|
Synonyms |
SER-LEU-ILE-GLY-ARG-LEU-AMIDE
H2N-SLIGRL-AMIDE Ser-Leu-Ile-Gly-Arg-Leu-NH2 SLIGRLAMIDE H-SER-LEU-ILE-GLY-ARG-LEU-NH2 PAR2-AP REF DUPL: H-Ser-Leu-Ile-Gly-Arg-Leu-NH2 SER-LEU-ILE-GLY-ARG-LEU-NH2 Protease-Activated Receptor-2 Activating Peptide |
Description | Protease-Activated Receptor-2 Activating Peptide is an agonist of Protease-Activated Receptor-2 (PAR-2). |
---|---|
Related Catalog | |
Target |
PAR-2[1] |
In Vitro | Protease-Activated Receptor-2 Activating Peptide (SLIGRL-NH2) is an agonist of PAR-2 and MrgprC11[1]. Protease-Activated Receptor-2 Activating Peptide (SLIGRL-NH2) causes an L-NAME-inhibited relaxation. Based on SLIGRL-NH2 causing a concentration-dependent relaxation with an EC50 of 10 µM in endothelium-free preparations in the presence of perivascular adipose tissue (PVAT) , 20 µM is used as a suitable ‘test’ concentration of peptide in subsequent experiments designed to evaluate the effects of potential inhibitors of ADRF release/action. In the endothelium-free aorta preparations, SLIGRL-NH2 causes a concentration-dependent relaxation in preparations only in the presence of PVAT [+PVAT, -ENDO (endothelium)][2]. |
Kinase Assay | Tissues are routinely contracted with 100 mM potassium chloride (KCl) to test their viability. Then, after re-equilibration for 20 min in fresh buffer, tissues are contracted with 1 µM of phenylephrine and a test concentration of 1 µM ACh is added and the presence or absence of a relaxant response is monitored to verify the presence or absence of an intact functional endothelium. The contractile response to phenylephrine is expressed as a percentage of the contractile response caused by 100 mM KCl (% KCl). Upon standardizing the preparation with the use of KCl and ACh, the effects of added SLIGRL-NH2, 2-furoyl-LIGRLO-NH2, LRGILS-NH2, LSIGRL-NH2 and 2-furoyl-OLRGIL-NH2 on the tension of the phenylephrine-contracted preparations (1 µM phenylephrine) is monitored for tissues with/without an intact endothelium and with/without adherent PVAT. Relaxation (%) is expressed as a percentage reduction of the plateau tension developed in the presence of phenylephrine. The effects of the inhibitors (L-NAME, ODQ, indomethacin, 4-aminopyridine, combined apamin + charybdotoxin, glibenclamide, genistein, H89 and catalase) are measured by treating the tissues with the inhibitors for 15 min before their contraction with 1 µM phenylephrine, then followed by the addition of test concentrations of SLIGRL-NH2, 2-furoyl-LIGRLO-NH2, LRGILS-NH2, LSIGRL-NH2 and 2-furoyl-OLRGIL-NH2. In most experiments evaluating a role for PAR2, SLIGRL-NH2 is used at a concentration of 20 µM to ensure selectivity for PAR2[2]. |
References |
Density | 1.342g/cm3 |
---|---|
Molecular Formula | C29H56N10O7 |
Molecular Weight | 656.81800 |
Exact Mass | 656.43300 |
PSA | 296.74000 |
LogP | 1.79430 |
Storage condition | 2-8℃ |
Safety Phrases | 22-24/25 |
---|