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

Protease Activated Receptor (PAR)

Thrombin receptors

Protease Activated Receptor (PAR)

Related Products

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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-10119R
    Vorapaxar (Standard)
    		Antagonist
    Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. 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 (Standard)
  • HY-14993R
    SCH79797 (Standard)
    		Antagonist
    SCH79797 (Standard) is the analytical standard of SCH79797. This product is intended for research and analytical applications. 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 (Standard)
  • HY-135907
    (Rac)-AZ8838
    		Antagonist
    (Rac)-AZ8838 (P69, Example 1) is a conformational antagonist of proteinase-activated receptor 2 (PAR2), which can be used for the study of pain and inflammation-related diseases.
    (Rac)-AZ8838
  • HY-119158
    VU0652925
    		Antagonist
    VU0652925, an analog of BMS986120, is a PAR4 antagonist, with IC50 values of 43 pM and 39.2 pM for PAC1 and P-selectin, respectively. VU0652925 is able to suppress GPIIbIIIa activation.
    VU0652925
  • HY-169817
    PAR-2-IN-2
    		Inhibitor
    PAR-2-IN-2 (compound P-596) is a protease-activated receptor 2 (PAR-2) inhibitor with an IC50 of 10.79 μM for SLIGKV and an IC50 of greater than 200 μM for Trypsin.
    PAR-2-IN-2
  • HY-107146R
    PZ-128 (Standard)
    		Antagonist
    PZ-128 (Standard) (P1pal-7 (Standard)) is the analytical standard of PZ-128 (HY-107146). This product is intended for research and analytical applications. 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 (Standard)
  • HY-108556AR
    RWJ-56110 dihydrochloride (Standard)
    		Inhibitor
    RWJ-56110 dihydrochloride (Standard) is the analytical standard of RWJ-56110 (dihydrochloride) (HY-108556A). This product is intended for research and analytical applications. RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
    RWJ-56110 dihydrochloride (Standard)
  • HY-174829
    7,4'-Dimethoxy-3-hydroxyflavone
    		Antagonist
    7,4'-Dimethoxy-3-hydroxyflavone is an orally active PAR4 antagonist. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation with an IC50 of 1.4 μM. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation and PAR4 signaling pathways, including NF-κB, Ca2+/protein kinase C, Akt, ERK and p38. 7,4'-Dimethoxy-3-hydroxyflavone prevents vascular PAR4 expression, endothelial dysfunction and ameliorates oxidative stress in Streptozotocin (STZ) (HY-13753)-induced diabetic mice. 7,4'-Dimethoxy-3-hydroxyflavone prevents thrombosis in mice without affecting bleeding time[1][2].
    7,4'-Dimethoxy-3-hydroxyflavone
  • HY-14994R
    SCH79797 dihydrochloride (Standard)
    		Antagonist
    SCH79797 (dihydrochloride) (Standard) is the analytical standard of SCH79797 (dihydrochloride). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Species Source
Protease Activated Receptor (PAR) Isoform Comparison

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