2. シグナル伝達
  3. GPCR/G Protein
  4. Protease Activated Receptor (PAR)
  5. PAR2 Isoform

PAR2

Protease Activated Receptor 2 (PAR2) is a self-activated G protein-coupled receptor and a cell surface receptor for trypsin-like proteases[1][2]. Mechanistically, proteolytic cleavage exposes a tethered ligand, and PAR2 activation engages Gαq-mediated calcium release, MAPK/ERK1/2 signaling, NFκB, AP1, Smad2, and β-arrestin-related pathways[1][3][4]. In human kidney tubular epithelial cells, PAR2 activation induces TNF, CSF2, MMP-9, PAI-1, and CTGF, supporting inflammatory and fibrotic pathway studies[3]. In glioblastoma cell lines, PAR2, but not PAR1, increased VEGF secretion through MAPK/ERK1/2 rather than PI3K/Akt signaling, highlighting isoform-specific experimental relevance[4]. In epithelial barrier models, PAR2 activation impaired keratinocyte tight junction integrity and reduced claudin-1, occludin, and ZO-1 expression[5]. Compared with PAR1 and PAR4, PAR2 requires distinct ligand and pathway evaluation because ligands can signal through multiple PAR2 pathways[1]. For experimental applications, PAR2 agonist peptides, radiolabeled 2-furoyl-LIGRL-NH2, antagonists, antibodies, and pepducins help define receptor activation, binding, selectivity, and inflammatory responses[1][6][7].

PAR2 関連製品 (25):

製品番号 製品名 製品効果 純度
  • 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.
  • HY-112558
    AZ3451 Antagonist 99.84%
    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  • 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.
  • 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..
  • HY-P1260
    FSLLRY-NH2 Inhibitor 99.89%
    FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-404056
    (R)-AZ8838 Antagonist
    (R)-AZ8838 is a competitive PAR2 antagonist with a pKi of  5.2 for human PAR2. (R)-AZ8838 exert anti-inflammatory effects in a rat model of PAR2 agonist-induced paw oedema.
  • HY-P0283
    Protease-Activated Receptor-2, amide Agonist 99.48%
    Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.
  • HY-123617
    AZ8838 Antagonist 99.30%
    AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2.
  • HY-117793
    I-191 Antagonist 99.14%
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
  • HY-120261
    GB-88 Inhibitor 98.66%
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM.
  • HY-148016
    I-287 Inhibitor 99.36%
    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.
  • HY-120528A
    GB-110 hydrochloride Agonist 99.86%
    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.
  • HY-124748A
    ENMD-1068 hydrochloride Antagonist 98.33%
    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.
  • HY-14350
    AC-55541 Agonist 99.40%
    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.
  • HY-124061
    GB83 Antagonist 99.80%
    GB83 is a potent PAR2 antagonist. GB83 reverses neutrophil elastase‐induced synovitis and pain. GB83 blocks the effect of MET-1 supernatant on NG neurons.
  • HY-P1310
    VKGILS-NH2 Agonist 99.00%
    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.
  • HY-P1260A
    FSLLRY-NH2 TFA Inhibitor 98.97%
    FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-120528
    GB-110 Agonist
    GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-138951
    AY77 Agonist
    AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release.
  • 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.