1. GPCR/G Protein
  2. Protease-Activated Receptor (PAR)

Protease-Activated Receptor-2 Activating Peptide 

Cat. No.: HY-P1308
Handling Instructions

Protease-Activated Receptor-2 Activating Peptide is an agonist of Protease-Activated Receptor-2 (PAR-2). Sequence: Ser-Leu-Ile-Gly-Arg-Leu-NH2;SLIGRL-NH2.

For research use only. We do not sell to patients.

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Protease-Activated Receptor-2 Activating Peptide Chemical Structure

Protease-Activated Receptor-2 Activating Peptide Chemical Structure

CAS No. : 171436-38-7

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Protease-Activated Receptor-2 Activating Peptide is an agonist of Protease-Activated Receptor-2 (PAR-2). Sequence: Ser-Leu-Ile-Gly-Arg-Leu-NH2;SLIGRL-NH2.

IC50 & 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].

Solvent & Solubility
In Vitro: 

10 mM in H2O

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5225 mL 7.6124 mL 15.2249 mL
5 mM 0.3045 mL 1.5225 mL 3.0450 mL
10 mM 0.1522 mL 0.7612 mL 1.5225 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[2]

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].

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

References
Molecular Weight

656.82

Formula

C₂₉H₅₆N₁₀O₇

CAS No.

171436-38-7

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Protease-Activated Receptor-2 Activating Peptide
Cat. No.:
HY-P1308
Quantity:

Protease-Activated Receptor-2 Activating Peptide

Cat. No.: HY-P1308