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-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-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
  • 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-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-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)
Cat. No. Product Name / Synonyms Species Source
Protease Activated Receptor (PAR) Isoform Comparison

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