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-P10577
    RAG8 peptide
    		Antagonist
    RAG8 peptide is an antagonist for protease-activated receptor 4 (PAR 4), which inhibits late-stage platelet activation, and reduces thrombosis without altering hemostasis or increasing bleeding risk. RAG8 peptide can be used for atherosclerosis research.
    RAG8 peptide
  • HY-P1312
    LRGILS-NH2
    		Control
    LRGILS-NH2 is a reverse-sequence protease-activated receptor-2 (PAR-2)-inactive, negative control, and SLIGRL-NH2 is a PAR-2-activating peptide.
    LRGILS-NH2
  • HY-P1311A
    RLLFT-NH2 TFA
    		Control
    RLLFT-NH2 TFA is a reversed amino acid sequence negative control peptide for TFLLR-NH2 (HY-P0226).
    RLLFT-NH2 TFA
  • HY-180244
    P2L-003
    		Antagonist
    P2L-003 is a selective PAR2 antagonist with an IC50 of 0.62 μM in HT-29 cells. P2L-003 blocks PAR2-mediated Ca2+ mobilization without affecting PAR1, PAR4, or ATP-mediated signaling and dose-dependently suppresses the downstream MAPK signaling cascades, including ERK1/2 and p38 phosphorylation. P2L-003 can be used for colon cancer research.
    P2L-003
  • HY-P1262A
    Parstatin(human) TFA
    		Agonist
    Parstatin(human) TFA, a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.
    Parstatin(human) TFA
  • HY-159895
    PAR4 antagonist 7
    		Antagonist
    PAR4 antagonist 7 (Compound 20f) is selective PAR4 antagonist (IC50: 1.72 nM). PAR4 antagonist 7 inhibits PAR4 agonist-induced platelet aggregation. PAR4 antagonist 7 has good metabolic stability. PAR4 antagonist 7 does not show a bleeding tendency in mice.
    PAR4 antagonist 7
  • HY-P1313A
    PAR 4 (1-6) TFA
    		Agonist
    PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is a fragment of protease-activated receptor 4 (PAR4). PAR 4 (1-6) TFA acts as a PAR4-specific agonist.
    PAR 4 (1-6) TFA
  • HY-181999
    PC8
    		Inhibitor
    PC8 is a selective dual inhibitor of PARP1/CDK6, with an IC50 of 0.126 μM for PARP1 and 0.197 μM for CDK6. PC8 does not alter PARP1 expression, but reduces the expression of its downstream target PAR. PC8 inhibits the canonical Wnt/β-catenin signaling pathway. PC8 induces intracellular ROS accumulation and exacerbates DNA damage. PC8 inhibits the proliferation of triple-negative breast cancer (TNBC) cells. PC8 can be used for the research of triple-negative breast cancer.
    PC8
  • HY-124748
    ENMD-1068
    		Antagonist
    ENMD-1068 is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 can be used in the study of endometriosis and liver fibrosis.
    ENMD-1068
  • HY-18200A
    Atopaxar hydrochloride
    		Antagonist
    Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease.
    Atopaxar hydrochloride
  • HY-111214
    K-14585
    		Antagonist
    K-14585 is a peptide competitive PAR2 antagonist. K-14585 inhibits PAR2-dependent IL-8 production, NF-κB phosphorylation, and p38 signaling. K-14585 reduces SLIGKV (PAR2 agonist peptide)-induced Ca2+ mobilisation in primary human keratinocytes.
    K-14585
  • HY-P1261
    Parstatin(mouse)
    		Agonist
    Parstatin(mouse), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.
    Parstatin(mouse)
  • HY-P2380
    PAR3 (1-6) (human)
    PAR3 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 1 (PAR1) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR3 and residues 39-44 of the full-length human sequence. PAR3 (1-6) activates p42/44 MAPK signaling in fibroblasts expressing PAR1, but not PAR3, an effect that can be blocked by the PAR1 antagonist RWJ 56110.
    PAR3 (1-6) (human)
  • HY-P5372
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2
    		Agonist
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2, a bioactive peptide, is a selective Protease activating receptor 1 (PAR-1) agonist over PAR-2. PAR-1 belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2
  • HY-P3259
    AY254
    		Agonist
    AY254 is an analogue of AY77 (HY-138951). AY254 is ERK-biased PAR2 agonist with an EC50 of 2 nM. AY254 relieves cytokine-induced caspase 3/8 activation. AY254 also promotes scratch-wound healing and induced IL-8 secretion via PAR2-ERK1/2 signaling
    AY254
  • HY-162762
    PAR-2 antagonist 1
    		Antagonist
    PAR-2 antagonist 1 (Compound 9a) is a protease-activated receptor 2 (PAR2) antagonist with an IC50 value of 0.9 μM. PAR-2 antagonist 1 can effectively inhibit the proliferation and migration of breast cancer cells.
    PAR-2 antagonist 1
  • HY-162408
    PAR4 antagonist 3
    		Inhibitor
    PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min.
    PAR4 antagonist 3
  • HY-108556
    RWJ-56110
    		Inhibitor
    RWJ-56110 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 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 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
    RWJ-56110
  • HY-108554
    Q94 hydrochloride
    		Antagonist
    Q94 hydrochloride, a selective PAR1 antagonist (IC50=916 nM), can selectively block PAR1/Gαq interaction and signalling. Q94 hydrochloride blocks PAR1-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation.
    Q94 hydrochloride
  • HY-10119AR
    Vorapaxar sulfate (Standard)
    		Antagonist
    Vorapaxar (sulfate) (Standard) is the analytical standard of Vorapaxar (sulfate). This product is intended for research and analytical applications. Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
    Vorapaxar sulfate (Standard)
Cat. No. Product Name / Synonyms Species Source
Protease Activated Receptor (PAR) Isoform Comparison

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