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-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.
    GB-110
  • HY-P2933
    Activated protein C
    		Inhibitor
    Activated protein C is an anticoagulant targeting coagulation factors Va and VIIIa. Activated protein C demonstrates cytoprotective effects through binding to endothelial cell protein C receptor (EPCR) and protease-activated receptor-1 (PAR-1), regulating gene expression, anti-inflammation, anti-apoptosis, and stabilizing endothelial barriers. Activated protein C is promising for research of diseases such as severe sepsis and ischemic stroke.
    Activated protein C
  • HY-146248A
    TFMU-ADPr triethylamine
    		Substrate
    TFMU-ADPr triethylamine 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 triethylamine 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 triethylamine 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 triethylamine 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 triethylamine is also applicable to COVID-19-related research.
    TFMU-ADPr triethylamine
  • HY-P5358
    YFLLRNP
    		Agonist 98.57%
    YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
    YFLLRNP
  • HY-105999B
    APC 366 TFA
    		Inhibitor ≥99.0%
    APC 366 (TFA) is an irreversible mast cell tryptase inhibitor. APC 366 (TFA) can be used for the research of allergic diseases.
    APC 366 TFA
  • HY-114164F
    Canine Thrombin
    Canine Thrombin is a Canine serine protease that plays a central role in blood coagulation. Canine Thrombin stimulates macrophages to polarize into a unique phenotype characterized by anti-inflammatory and pro-repair properties. Canine Thrombin activates PAR1, induces the production of MCP-1, MMP3 and VEGF in intervertebral discs, and causes degradation of the cartilage matrix and destruction of intervertebral disc structure. Canine Thrombin activity increases significantly in paraoxon-induced status epilepticus.
    Canine Thrombin
  • HY-108555
    FR-171113
    		Antagonist
    FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM..
    FR-171113
  • HY-138951
    AY77
    		Agonist
    AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release.
    AY77
  • HY-143315
    Protease-Activated Receptor-1 antagonist 3
    		Antagonist
    Protease-Activated Receptor-1 antagonist 3 is a potent protease-activated receptor-1 antagonist with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 3 shows binding affinity for hERG K+ channel with an IC50 value of 9 µM.
    Protease-Activated Receptor-1 antagonist 3
  • HY-W006069
    H-Phe(3,5-DiF)-OH
    H-Phe(3,5-DiF)-OH is a difluorophenylalanines in the L-configuration [L-(F2)Phe]. H-Phe(3,5-DiF)-OH can be incorporated into the thrombin receptor-tethered ligand peptide SFLLRNP to identify the phenyl hydrogens of the Phe-2 residue involved in the CH/π receptor interaction.
    H-Phe(3,5-DiF)-OH
  • 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).
    Thrombin Receptor Activator for Peptide 5 (TRAP-5)
  • HY-163504
    PAR4 antagonist 5
    		Antagonist
    PAR4 antagonist 5 (compound 1) is a PAR4 antagonist with an IC50 less than 20 μM and potent anti-platelet aggregation activity. PAR4 antagonist 5 can be used for research of thrombosis disease .
    PAR4 antagonist 5
  • HY-146248
    TFMU-ADPr
    		Substrate
    TFMU-ADPr 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 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 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 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 is also applicable to COVID-19-related research.
    TFMU-ADPr
  • HY-18201
    SCH-602539
    		Antagonist
    SCH-602539 is a selective PAR-1 antagonist. SCH-602539 inhibits platelet aggregation in response to PAR-1-selective high-affinity thrombin receptor agonist peptide. SCH-602539 exhibits synergistic antithrombotic effects when used in combination with Cangrelor (HY-19638).
    SCH-602539
  • HY-P4451
    TRAP-5 amide
    		Agonist
    TRAP-5 amide is a protease-activated receptor 1 (PAR 1) agonist peptide.
    TRAP-5 amide
  • HY-10119S
    Vorapaxar-d5
    		Antagonist
    Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). 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-d<sub>5</sub>
  • HY-162409
    PAR4 antagonist 4
    		Inhibitor
    PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min.
    PAR4 antagonist 4
  • HY-P2519
    Protease-Activated Receptor-3 (PAR-3) (1-6), human
    		Agonist
    Protease-Activated Receptor-3 (PAR-3) (1-6), human is a proteinase-activated receptor (PAR-3) agonist peptide.
    Protease-Activated Receptor-3 (PAR-3) (1-6), human
  • HY-161401
    PAR4 antagonist 2
    		Antagonist
    PAR4 antagonist 2 (Compound 31) is a protease activated receptor 4 (PAR4) antagonist, with IC50 values of 95 nM and 367 nM for human PAR4 and mouse PAR4. PAR4 antagonist 2 is active against PAR4 activation by the native protease thrombin cleavage but not the synthetic PAR4 agonist peptide AYPGKF.
    PAR4 antagonist 2
  • HY-163341
    PAR4 antagonist 1
    		Antagonist
    PAR4 antagonist 1 (Compound 48) is a protease activated receptor 4 (PAR4) antagonist with an IC50 of 1.8 nM. PAR4 antagonist 1 has an IC50 of 2 nM against γ-thrombin-activated PAR4 in platelet-rich plasma (PRP). PAR4 antagonist 1 can be used in antithrombotic research.
    PAR4 antagonist 1
Cat. No. Product Name / Synonyms Species Source
Protease Activated Receptor (PAR) Isoform Comparison

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