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

Protease Activated Receptor (PAR)

Thrombin receptors

Protease Activated Receptor (PAR)

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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.

Protease Activated Receptor (PAR) Isoform Specific Products:

Protease Activated Receptor (PAR) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-129047
    Trypsin
    		Activator
    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.
    Trypsin
  • HY-P0078
    TRAP-6
    		Agonist 99.98%
    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.
    TRAP-6
  • HY-10119
    Vorapaxar
    		Antagonist 99.61%
    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.
    Vorapaxar
  • HY-112558
    AZ3451
    		Antagonist 99.84%
    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
    AZ3451
  • HY-P1308
    SLIGRL-NH2
    		Agonist 99.39%
    SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is an agonist of Protease-Activated Receptor-2 (PAR-2).
    SLIGRL-NH2
  • HY-182573
    RWJ-58259
    		Antagonist
    RWJ-58259 is a selective PAR-1 inhibitor with an IC50 value of 0.15 μM. RWJ-58259 binds selectively to PAR-1, blocks the binding of tethered ligands, interferes with calcium mobilization and PAR-1-related cellular functions, and exhibits no PAR-1 agonist activity or thrombin proteolytic inhibitory activity. RWJ-58259 inhibits thrombin-induced platelet aggregation, calcium signaling and vascular smooth muscle cell proliferation, reduces neointimal thickness and arterial stenosis, and alleviates vascular occlusion and platelet deposition. RWJ-58259 can be used in the research of thrombotic diseases and vascular injury associated with acute coronary intervention.
    RWJ-58259
  • HY-171096
    PAR2 modulator-1
    		Antagonist
    PAR2 modulator-1 (Compound C781) is a protease activated receptor type 2 (PAR2) antagonist. PAR2 modulator-1 can specifically inhibit the PAR2-dependent MAPK signaling pathway with an IC50 value of 8.5 μM. PAR2 modulator-1 can block the pain response triggered by PAR2 agonists. PAR2 modulator-1 can be used for the researches of inflammation, immunology and neurological disease, such as chronic pain and asthma.
    PAR2 modulator-1
  • HY-P991988
    Anti-PAR1 Antibody
    		Inhibitor
    Anti-PAR1 Antibody is an anti-PAR1 antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-PAR1 Antibody
  • HY-129047A
    Trypsin (MS grade)
    		Activator
    Trypsin MS grade is a serine protease enzyme, and hydrolyzes proteins at the carboxyl side of the Lysine or Arginine. Trypsin MS grade activates PAR2 and PAR4. Trypsin MS grade induces cell-to-cell membrane fusion in PDCoV infection by the interaction of S glycoprotein of PDCoV and pAPN. Trypsin MS grade also promotes cell proliferation and differentiation. Trypsin MS grade can be used in the research of wound healing and neurogenic inflammation.
    Trypsin (MS grade)
  • HY-P1309
    PAR-4 Agonist Peptide, amide
    		Agonist 99.75%
    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.
    PAR-4 Agonist Peptide, amide
  • 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..
    2-Furoyl-LIGRLO-amide
  • HY-19837
    BMS-986120
    		Antagonist 98.22%
    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.
    BMS-986120
  • HY-P1260
    FSLLRY-NH2
    		Inhibitor 99.89%
    FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
    FSLLRY-NH2
  • HY-14993
    SCH79797
    		Antagonist 99.74%
    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.
    SCH79797
  • HY-P0283
    Protease-Activated Receptor-2, amide
    		Agonist 99.48%
    Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.
    Protease-Activated Receptor-2, amide
  • HY-13965
    Parmodulin 2
    		Inhibitor 99.82%
    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.
    Parmodulin 2
  • HY-123617
    AZ8838
    		Antagonist 99.30%
    AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2.
    AZ8838
  • HY-117793
    I-191
    		Antagonist 99.14%
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
    I-191
  • HY-120261
    GB-88
    		Inhibitor 98.66%
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM.
    GB-88
  • HY-146248B
    TFMU-ADPr diammonium
    		Substrate 98.78%
    TFMU-ADPr diammonium is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr diammonium can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr diammonium binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr diammonium can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr diammonium is also applicable to COVID-19-related research.
    TFMU-ADPr diammonium
Cat. No. Product Name / Synonyms Species Source
Protease Activated Receptor (PAR) Isoform Comparison

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