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

Protease Activated Receptor (PAR) Antagonist

Protease Activated Receptor (PAR) Antagonists (16):

Cat. No. Product Name Effect Purity
  • 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.
  • 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-171096
    PAR2 modulator-1
    		Antagonist
    PAR2 modulator-1 (Compound C781) is a protease activated receptor type 2 (PAR2) antagonist. PAR2 modulator-1 can specifically inhibit the PAR2-dependent MAPK signaling pathway with an IC50 value of 8.5 μM. PAR2 modulator-1 can block the pain response triggered by PAR2 agonists. PAR2 modulator-1 can be used for the researches of inflammation, immunology and neurological disease, such as chronic pain and asthma.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • HY-120544
    BAY-386
    		Antagonist
    BAY-386, a chemical probe, is a PAR-1 antagonist that inhibits the expression of pro-inflammatory factors MCP-1 and CXCL1 in HUVEC.
  • HY-159896
    PAR4 antagonist 8
    		Antagonist
    PAR4 antagonist 8 (Compound 20f) is an effective, orally active, and selective PAR4 antagonist with an IC50 value of 15.32 nM. PAR4 antagonist 8 exhibits favorable pharmacokinetic properties. PAR4 antagonist 8 not only effectively inhibits human platelet aggregation induced by PAR4 agonists (IC50 = 6.39 nM) but also inhibits mouse platelet aggregation. PAR4 antagonist 8 can be used in antithrombotic research.
  • HY-10119R
    Vorapaxar (Standard)
    		Antagonist
    Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. 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-14993R
    SCH79797 (Standard)
    		Antagonist
    SCH79797 (Standard) is the analytical standard of SCH79797. This product is intended for research and analytical applications. 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-135907
    (Rac)-AZ8838
    		Antagonist
    (Rac)-AZ8838 (P69, Example 1) is a conformational antagonist of proteinase-activated receptor 2 (PAR2), which can be used for the study of pain and inflammation-related diseases.
  • HY-119158
    VU0652925
    		Antagonist
    VU0652925, an analog of BMS986120, is a PAR4 antagonist, with IC50 values of 43 pM and 39.2 pM for PAC1 and P-selectin, respectively. VU0652925 is able to suppress GPIIbIIIa activation.
  • HY-107146R
    PZ-128 (Standard)
    		Antagonist
    PZ-128 (Standard) (P1pal-7 (Standard)) is the analytical standard of PZ-128 (HY-107146). This product is intended for research and analytical applications. 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-14994R
    SCH79797 dihydrochloride (Standard)
    		Antagonist
    SCH79797 (dihydrochloride) (Standard) is the analytical standard of SCH79797 (dihydrochloride). This product is intended for research and analytical applications. 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.