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

Protease Activated Receptor (PAR) Antagonist

Protease Activated Receptor (PAR) Isoform Comparison

Protease Activated Receptor (PAR) Antagonists (42):

Cat. No. Product Name Effect Purity
  • 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.
  • HY-112558
    AZ3451
    		Antagonist 99.84%
    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.
  • HY-P5875A
    P4pal10 TFA
    		Antagonist 98.25%
    P4pal10 TFA is the TFA salt form of P4pal10 (HY-P5875). P4pal10 TFA is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 TFA inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 TFA reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 TFA ameliorates the injury in rats myocardial ischemia/reperfusion (I/R) models.
  • HY-159632
    PAR4 antagonist 6
    		Antagonist
    PAR4 antagonist 6 (Compound 12) is a PAR4 antagonist, with IC50 values of 134 and 401 nM for hPAR4 (PAC1) and mPAR4 (PAC1), respectively.
  • HY-19837
    BMS-986120
    		Antagonist 98.54%
    BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects.
  • HY-14993
    SCH79797
    		Antagonist 99.74%
    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.
  • 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.
  • HY-10119A
    Vorapaxar sulfate
    		Antagonist 99.81%
    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.
  • HY-117793
    I-191
    		Antagonist 99.14%
    I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.
  • HY-107146
    PZ-128
    		Antagonist 99.47%
    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.
  • 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-14994
    SCH79797 dihydrochloride
    		Antagonist 99.91%
    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.
  • HY-18200
    Atopaxar
    		Antagonist 99.83%
    Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease.
  • HY-P1263A
    tcY-NH2 TFA
    		Antagonist 99.72%
    tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) TFA is a potent selective PAR4 antagonist peptide. tcY-NH2 TFA inhibits thrombin- and AY-NH2-induced platelet aggregation and endostatin release, and can be used in the research of inflammation, immunology.
  • HY-150790
    BMS-986141
    		Antagonist 98.86%
    BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect.
  • HY-P5359
    FLLRN
    		Antagonist 98.99%
    FLLRN is a biological active peptide. (PAR1-specific antagonist peptide)
  • 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-19973
    ML354
    		Antagonist 98.80%
    ML354 is a selective PAR4 antagonist with an IC50 of 140 nM.
  • HY-108555
    FR-171113
    		Antagonist
    FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM..
  • HY-143315
    Protease-Activated Receptor-1 antagonist 3
    		Antagonist
    Protease-Activated Receptor-1 antagonist 3 is a potent protease-activated receptor-1 antagonist with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 3 shows binding affinity for hERG K+ channel with an IC50 value of 9 µM.