1. Signaling Pathways
  2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)

Protease Activated Receptor (PAR)

Thrombin receptors

Protease activated receptors (PARs) are a family of G-protein-coupled receptors (GPCRs) that are irreversibly activated by proteolytic cleavage of the N terminus, which unmasks a tethered peptide ligand that binds and activates the transmembrane receptor domain, eliciting a cellular cascade in response to inflammatory signals and other stimuli. There are four members of the PAR family: PAR1, PAR2, PAR3 and PAR4. PARs have important functions in the vasculature, inflammation, and cancer and are important drug targets.

PARs are expressed on nearly all cell types in the blood vessel wall (ECs, fibroblasts, myocytes) and blood (platelets, neutrophils, macrophages, leukemic white cells) with exception of red blood cells. Thrombin-activated PAR-1, PAR-3, and PAR-4 are also expressed in epithelium, neurons, astrocytes, and immune cells. PAR-2, which is activated by trypsin-like serine proteases, is found in human vascular, intestinal, neuronal, and airway cells. Its expression increases in injured tissues or after stimulation by inflammatory mediators.

Cat. No. Product Name Effect Purity
  • HY-10119
    Antagonist 99.85%
    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
    Agonist 99.84%
    TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4.
  • HY-112558
    Antagonist 99.60%
    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  • HY-P1308
    Agonist 99.78%
    SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • 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-P5001
    Agonist 99.26%
    iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. iso-TRAP-6 is an analog of TRAP-6 (HY-P0078) that refers to the use of isoserine instead of serine as first amino acid.
  • HY-P5359
    Antagonist 98.99%
    FLLRN is a biological active peptide. (PAR1-specific antagonist peptide)
  • HY-P4451
    TRAP-5 amide
    TRAP-5 amide is a protease-activated receptor 1 (PAR 1) agonist peptide.
  • HY-129047
    Trypsin is a serine protease enzyme, and hydrolyzes proteins at the carboxyl side of the Lysine or Arginine. Trypsin activates PAR2 and PAR4. Trypsin induces cell-to-cell membrane fusion in PDCoV infection by the interaction of S glycoprotein of PDCoV and pAPN. Trypsin also promotes cell proliferation and differentiation. Trypsin can be used in the research of wound healing and neurogenic inflammation.
  • HY-P1314
    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-120261
    Inhibitor 99.05%
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 µM.
  • HY-P0283
    Protease-Activated Receptor-2, amide
    Agonist 99.33%
    Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.
  • HY-14993
    Antagonist 99.83%
    SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 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 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
  • HY-120528A
    GB-110 hydrochloride
    Agonist 99.83%
    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-19837
    Antagonist 98.54%
    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 98.26%
    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-P1260A
    Inhibitor 99.43%
    FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-14350
    Agonist 99.25%
    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
    Antagonist 99.38%
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
  • HY-107146
    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.
Cat. No. Product Name / Synonyms Species Source