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

Protease-Activated Receptor (PAR)

Protease activated receptors (PARs) are a family of four G-protein-coupled receptors (PAR1, PAR2, PAR3, and PAR4) that are self-activated by tethered peptide ligands exposed by proteolytic cleavage of the extracellular amino terminus. PAR1, PAR3, and PAR4 are activated by thrombin, whereas PAR2 and, to a lesser degree, PAR4, are activated by trypsin.

PAR1 is a thrombin-activated receptor that contributes to inflammatory responses at mucosal surfaces. PAR1 antagonism might be explored as a treatment for influenza, including that caused by highly pathogenic H5N1 and oseltamivir-resistant H1N1 viruses.

PAR2 receptors have been implicated in numerous physiological processes necessitating therapeutic intervention, especially pain and inflammation and syndromes with a strong inflammatory component, including colitis, gastritis, pancreatitis, asthma and pulmonary disease, and arthritis.

Protease-Activated Receptor (PAR) Related Products (6):

Cat. No. Product Name Effect Purity
  • HY-10119
    Vorapaxar Antagonist 99.90%
    Vorapaxar is a thrombin receptor (protease-activated receptor, PAR-1) antagonist.
  • HY-P0078
    TRAP-6 Agonist 99.82%
    TRAP-6 is protease-activated receptor 1 (PAR1) agonist.
  • HY-14350
    AC-55541 Agonist 99.35%
    AC-55541 is a novel small-molecule protease-activated receptor 2(PAR2) agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2(addition)) mobilization assays, with potencies ranging from 200 to 1000 nM.
  • HY-P0226
    TFLLR-NH2 Agonist
    TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.
  • HY-P0297
    Protease-Activated Receptor-4 Agonist
    Protease-Activated Receptor-4 is the agonist of proteinase-activated receptor-4 (PAR4).
  • HY-P0283
    Protease-Activated Receptor-2, amide Agonist
    Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.