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-10119
    Vorapaxar
    		Antagonist 99.85%
    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
  • HY-P0078
    TRAP-6
    		Agonist 99.84%
    TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4.
    TRAP-6
  • HY-129047
    Trypsin
    		Activator
    Trypsin is a serine protease enzyme, and hydrolyzes proteins at the carboxyl side of the Lysine or Arginine. Trypsin activates PAR2 and PAR4. Trypsin induces cell-to-cell membrane fusion in PDCoV infection by the interaction of S glycoprotein of PDCoV and pAPN. Trypsin also promotes cell proliferation and differentiation. Trypsin can be used in the research of wound healing and neurogenic inflammation.
    Trypsin
  • HY-112558
    AZ3451
    		Antagonist 99.84%
    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
    AZ3451
  • HY-P1308
    SLIGRL-NH2
    		Agonist 99.78%
    SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is an agonist of Protease-Activated Receptor-2 (PAR-2).
    SLIGRL-NH2
  • HY-P4451
    TRAP-5 amide
    		Agonist
    TRAP-5 amide is a protease-activated receptor 1 (PAR 1) agonist peptide.
    TRAP-5 amide
  • 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-P4987
    TRAP-7
    		Activator
    TRAP-7 is a thrombin receptor (PAR) activating peptide. TRAP-7 stimulates total inositol phosphate (IP) accumulation and phosphorylation of a specific endogenous substrate for activated PKC. TRAP-7 can be used in cardiovascular disease research.
    TRAP-7
  • HY-P1309A
    PAR-4 Agonist Peptide, amide TFA
    		Agonist 99.93%
    PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) 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 TFA
  • HY-P1314
    2-Furoyl-LIGRLO-amide
    		Agonist 99.87%
    2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0..
    2-Furoyl-LIGRLO-amide
  • HY-14993
    SCH79797
    		Antagonist 99.83%
    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
  • HY-P0283
    Protease-Activated Receptor-2, amide
    		Agonist 99.33%
    Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.
    Protease-Activated Receptor-2, amide
  • HY-120261
    GB-88
    		Inhibitor 99.05%
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 µM.
    GB-88
  • HY-120528A
    GB-110 hydrochloride
    		Agonist 99.83%
    GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.
    GB-110 hydrochloride
  • HY-123617
    AZ8838
    		Antagonist 98.87%
    AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2.
    AZ8838
  • HY-P1260A
    FSLLRY-NH2 TFA
    		Inhibitor 99.43%
    FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
    FSLLRY-NH2 TFA
  • HY-13965
    Parmodulin 2
    		Inhibitor 98.26%
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
    Parmodulin 2
  • HY-117793
    I-191
    		Antagonist 99.38%
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
    I-191
  • HY-10119A
    Vorapaxar sulfate
    		Antagonist 99.40%
    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
  • HY-14350
    AC-55541
    		Agonist 99.25%
    AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. AC-55541 has pEC50 values of 5.9 and 6.6 in PI hydrolysis assays and Ca2+ mobilization assays and exhibits pronociceptive activity in vivo.
    AC-55541
Cat. No. Product Name / Synonyms Species Source