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 (32):

Cat. No. Product Name Effect Purity
  • HY-10119
    Vorapaxar Antagonist 99.91%
    Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
  • HY-P0078
    TRAP-6 Agonist 99.74%
    TRAP-6 (PAR-1 agonist peptide) is a protease-activated receptor 1 (PAR1) agonist.
  • HY-112558
    AZ3451 Antagonist 99.33%
    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 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.
  • HY-P0226A
    TFLLR-NH2(TFA) Agonist 99.29%
    TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM.
  • HY-124748A
    ENMD-1068 hydrochloride Antagonist 98.18%
    ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist with antiangiogenic and anti-inflammatory activities. ENMD-1068 hydrochloride reduces epatic stellate cells (HSCs) activation and collagen expression through the inhibiton of TGF-β1/Smad signal transduction.
  • HY-107146
    PZ-128 Antagonist 99.47%
    PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects.
  • HY-P1263A
    tcY-NH2 TFA Antagonist 99.84%
    tcY-NH2 TFA is a selective rat PAR4 antagonist peptide. tcY-NH2 TFA inhibits thrombin- and AY-NH2-induced rat platelet aggregation.
  • HY-P1309A
    PAR-4 Agonist Peptide, amide TFA Agonist 99.97%
    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-14350
    AC-55541 Agonist 99.19%
    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-117793
    I-191 Antagonist 98.02%
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
  • HY-14994
    SCH79797 dihydrochloride Antagonist >99.0%
    SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
  • HY-13965
    Parmodulin 2 Inhibitor 98.03%
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
  • HY-P1314
    2-Furoyl-LIGRLO-amide Agonist 99.87%
    2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0..
  • HY-120528A
    GB-110 hydrochloride Agonist 99.94%
    GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-P1308
    SLIGRL-NH2 Agonist 99.66%
    SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • HY-120261
    GB-88 Inhibitor 98.78%
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 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-P1260
    FSLLRY-NH2 Inhibitor
    FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
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