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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    PZ-128
  • HY-124748A
    ENMD-1068 hydrochloride
    		Antagonist 98.56%
    ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis.
    ENMD-1068 hydrochloride
  • HY-14994
    SCH79797 dihydrochloride
    		Antagonist 99.91%
    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.
    SCH79797 dihydrochloride
  • HY-P0226A
    TFLLR-NH2(TFA)
    		Agonist 99.78%
    TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM.
    TFLLR-NH2(TFA)
  • HY-18200
    Atopaxar
    		Antagonist 98.05%
    Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease.
    Atopaxar
  • HY-P1260
    FSLLRY-NH2
    		Inhibitor 98.52%
    FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
    FSLLRY-NH2
  • HY-P0297
    Protease-Activated Receptor-4
    		Agonist
    Protease-Activated Receptor-4 is the agonist of proteinase-activated receptor-4 (PAR4).
    Protease-Activated Receptor-4
  • HY-138558
    PAR-2-IN-1
    		Inhibitor 99.79%
    PAR-2-IN-1 is a protease-activated receptor-2 (PAR2) signaling pathway inhibitor with anti-inflammatory and anticancer effects.
    PAR-2-IN-1
  • HY-P1309
    PAR-4 Agonist Peptide, amide
    		Agonist 99.48%
    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-P1310
    VKGILS-NH2
    		Agonist 99.81%
    VKGILS-NH2 is a reversed amino acid sequence control peptide for SLIGKV-NH2 (protease-activated receptor 2 (PAR2) agonist). VKGILS-NH2 has no effect on DNA synthesis in cells.
    VKGILS-NH2
  • HY-P1263A
    tcY-NH2 TFA
    		Antagonist 99.72%
    tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) TFA is a potent selective PAR4 antagonist peptide. tcY-NH2 TFA inhibits thrombin- and AY-NH2-induced platelet aggregation and endostatin release, and can be used in the research of inflammation, immunology.
    tcY-NH2 TFA
  • HY-P4803
    PAR-2 (1-6) (human)
    		Agonist 99.49%
    PAR-2 (1-6) (human) (SLIGKV), a peptide ligand, is a PAR-2 agonist.
    PAR-2 (1-6) (human)
  • HY-P2519A
    Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA
    		Agonist 99.86%
    Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a proteinase-activated receptor (PAR-3) agonist peptide.
    Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA
  • HY-P2518A
    Protease-Activated Receptor-1, PAR-1 Agonist TFA
    		Agonist 98.54%
    Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor.
    Protease-Activated Receptor-1, PAR-1 Agonist TFA
  • 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-P2518
    Protease-Activated Receptor-1, PAR-1 Agonist
    		Agonist 98.34%
    Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor.
    Protease-Activated Receptor-1, PAR-1 Agonist
  • HY-P5001
    iso-TRAP-6
    		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.
    iso-TRAP-6
  • HY-14351
    AC-264613
    		Agonist 98.15%
    AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC50 of 7.5.
    AC-264613
  • HY-148016
    I-287
    		Inhibitor
    I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research.
    I-287
  • HY-P1261A
    Parstatin(mouse) TFA
    		Agonist 99.71%
    Parstatin(mouse) TFA, a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.
    Parstatin(mouse) TFA
Cat. No. Product Name / Synonyms Species Source