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 (12):

Cat. No. Product Name Effect Purity
  • HY-10119
    Vorapaxar Antagonist 99.91%
    Vorapaxar is a protease-activated receptor (PAR-1) antagonist that inhibits thrombin-induced platelet activation.
  • HY-P0078
    TRAP-6 Agonist 99.84%
    TRAP-6 is a protease-activated receptor 1 (PAR1) agonist. Sequence: Ser-Phe-Leu-Leu-Arg-Asn;SFLLRN.
  • HY-112558
    AZ3451 Antagonist 99.13%
    AZ3451 is a protease-activated receptor-2 (PAR2) antagonist.
  • 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-P0283
    Protease-Activated Receptor-2, amide Agonist 98.33%
    Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide. Sequence: Ser-Leu-Ile-Gly-Lys-Val-NH2;SLIGKV-NH2.
  • HY-P0226A
    TFLLR-NH2(TFA) Agonist 99.29%
    TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM. Sequence: Thr-Phe-Leu-Leu-Arg-NH2;TFLLR-NH2.
  • HY-19837
    BMS-986120 Antagonist
    BMS-986120 is an antagonist of the Platelet Protease-Activated Receptor-4 (PAR4), with IC50s of 9.5, 2.1 nM in human and monkey blood, respectively.
  • HY-P0297
    Protease-Activated Receptor-4 Agonist 98.35%
    Protease-Activated Receptor-4 is the agonist of proteinase-activated receptor-4 (PAR4). Sequence: Gly-Tyr-Pro-Gly-Lys-Phe-NH2;GYPGKF-NH2.
  • HY-P0226
    TFLLR-NH2 Agonist
    TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM. Sequence: Thr-Phe-Leu-Leu-Arg-NH2;TFLLR-NH2.
  • HY-P1536
    Thrombin Receptor Activator for Peptide 5 TRAP-5
    Thrombin Receptor Activator for Peptide 5 (TRAP-5) is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD). Sequence: Ser-Phe-Leu-Leu-Arg;SFLLR.
  • HY-P1309
    PAR-4 Agonist Peptide, amide Agonist
    PAR-4 Agonist Peptide, amide is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist. Sequence: Ala-Tyr-Pro-Gly-Lys-Phe-NH2;AYPGKF-NH2.
  • HY-P1308
    Protease-Activated Receptor-2 Activating Peptide Agonist
    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.