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

Protease-Activated Receptor-2, amide 

Cat. No.: HY-P0283 Purity: 98.33%
Handling Instructions

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

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

Custom Peptide Synthesis

Protease-Activated Receptor-2, amide Chemical Structure

Protease-Activated Receptor-2, amide Chemical Structure

CAS No. : 190383-13-2

Size Price Stock Quantity
10 mM * 1  mL in Water USD 114 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
25 mg USD 264 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

PAR2[1]

In Vitro

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].

Molecular Weight

614.78

Formula

C₂₈H₅₄N₈O₇

CAS No.

190383-13-2

Sequence

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

Sequence Shortening

SLIGKV-NH2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 33.33 mg/mL (54.21 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6266 mL 8.1330 mL 16.2660 mL
5 mM 0.3253 mL 1.6266 mL 3.2532 mL
10 mM 0.1627 mL 0.8133 mL 1.6266 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

Protease-Activated Receptor-2, amideProtease-Activated Receptor (PAR)Thrombin receptorsInhibitorinhibitorinhibit

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Protease-Activated Receptor-2, amide
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HY-P0283
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