1. Signaling Pathways
  2. GPCR/G Protein
  3. 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 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 (18):

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-112558
    AZ3451 Antagonist 99.33%
    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  • HY-P0078
    TRAP-6 Agonist 99.84%
    TRAP-6 is a protease-activated receptor 1 (PAR1) agonist.
  • HY-14350
    AC-55541 Agonist 99.35%
    AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. AC-55541 has pEC50 values of 5.9 and 6.6 in PI hydrolysis assays and Ca2+ mobilization assays and exhibits pronociceptive activity in vivo.
  • 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.
  • HY-P1309A
    PAR-4 Agonist Peptide, amide TFA Agonist 99.93%
    PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) 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.
  • HY-120528
    GB-110 Agonist
    GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-117793
    I-191 Antagonist 98.02%
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
  • HY-P0226A
    TFLLR-NH2(TFA) Agonist 99.29%
    TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM.
  • HY-P0297
    Protease-Activated Receptor-4 Agonist 98.35%
    Protease-Activated Receptor-4 is the agonist of proteinase-activated receptor-4 (PAR4).
  • HY-P0226
    TFLLR-NH2 Agonist
    TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.
  • HY-19837
    BMS-986120 Antagonist
    BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects.
  • HY-13965
    Parmodulin 2 Inhibitor
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) and has shown cytoprotective effects in cellular and animal studies. Parmodulin 2 also significantly decreases cardiac infarct size in a murine model of myocardial ischemia–reperfusion injury.
  • HY-128345
    UDM-001651 Antagonist
    UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP).
  • 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).
  • HY-P1309
    PAR-4 Agonist Peptide, amide Agonist
    PAR-4 Agonist Peptide, amide (PAR-4-AP; AY-NH2) 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.
  • 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).
  • HY-120261
    GB-88 Inhibitor
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 µM.
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