Protease Activated Receptor (PAR)
Thrombin receptors
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
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Protease Activated Receptor (PAR) Inhibitors
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Protease Activated Receptor (PAR) Agonists
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Protease Activated Receptor (PAR) Antagonists
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Protease Activated Receptor (PAR) Activators
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Protease Activated Receptor (PAR) Controls
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Protease Activated Receptor (PAR) Substrates
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Protease-activated Receptor Proteins
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Protease Activated Receptor (PAR) Related Products (136)
Related Products (136)
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Recombinant Proteins (2)
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Protease Activated Receptor (PAR) Isoform Comparison
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TRAP-6 amide TFA
0 ImagesCat. No.: HY-P2321ACAS No.: 1426807-16-0TRAP-6 amide TFA is a PAR-1 thrombin receptor agonist peptide.
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TRAP-6-IN-1
0 ImagesCat. No.: HY-146333CAS No.: 2068737-10-8
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TRAP-14 amide
0 ImagesCat. No.: HY-P5764CAS No.: 141923-36-6TRAP-14 amide, a proteinase activated receptor (PAR)-activating peptide, is a PAR agonist with an EC50 of 24 μM. TRAP-14 amide significantly induces platelet aggregation through ADP- and MMP-2-dependent pathways with Aspirin (HY-14654)-insensitivity. TRAP-14 amide also effectively increases glycoprotein (GP) Ib and GPIIb/IIIa surface expression and ADP release.
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SLIGRL-NH2 TFA
0 ImagesCat. No.: HY-P1308ACAS No.: 2828432-39-7Synonyms: Protease-Activated Receptor-2 Activating Peptide TFASLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) is an agonist of Protease-Activated Receptor-2 (PAR-2).
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Atopaxar hydrobromide
0 ImagesCat. No.: HY-18200BCAS No.: 474550-69-1Synonyms: E5555 hydrobromide; ER 172594-06Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease.
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PAR4 antagonist 8
0 ImagesCat. No.: HY-159896PAR4 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.
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Vorapaxar (Standard)
0 ImagesSynonyms: SCH 530348 (Standard)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.
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SCH79797 (Standard)
0 ImagesCat. No.: HY-14993RCAS No.: 245520-69-8SCH79797 (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.
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(Rac)-AZ8838
0 ImagesCat. No.: HY-135907CAS No.: 2100283-63-2
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VU0652925
0 ImagesCat. No.: HY-119158CAS No.: 1476847-58-1VU0652925, 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.
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PAR-2-IN-2
0 ImagesCat. No.: HY-169817CAS No.: 313986-65-1PAR-2-IN-2 (compound P-596) is a protease-activated receptor 2 (PAR-2) inhibitor with an IC50 of 10.79 μM for SLIGKV and an IC50 of greater than 200 μM for Trypsin.
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PZ-128 (Standard)
0 ImagesCat. No.: HY-107146RCAS No.: 371131-16-7Synonyms: P1pal-7 (Standard)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.
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SC42619 free base
0 ImagesCat. No.: HY-123200CAS No.: 107534-95-2SC42619 free base is a selective platelet thrombin receptor (thrombin receptor) antagonist. SC42619 free base inhibits thrombin-induced platelet aggregation, secretion, calcium influx, and phosphatidic acid phosphorylation, as well as trypsin-induced platelet aggregation. SC42619 free base reduces the content of individual platelets. SC42619 free base inhibits prostacyclin (PGI2) synthesis in endothelial cells. SC42619 free base can be used for the research of hematological diseases.
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RWJ-56110 dihydrochloride (Standard)
0 ImagesCat. No.: HY-108556ARCAS No.: 2387505-58-8RWJ-56110 dihydrochloride (Standard) is the analytical standard of RWJ-56110 (dihydrochloride) (HY-108556A). This product is intended for research and analytical applications. RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
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7,4'-Dimethoxy-3-hydroxyflavone
0 ImagesCat. No.: HY-174829CAS No.: 13198-99-77,4'-Dimethoxy-3-hydroxyflavone is an orally active PAR4 antagonist. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation with an IC50 of 1.4 μM. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation and PAR4 signaling pathways, including NF-κB, Ca2+/protein kinase C, Akt, ERK and p38. 7,4'-Dimethoxy-3-hydroxyflavone prevents vascular PAR4 expression, endothelial dysfunction and ameliorates oxidative stress in Streptozotocin (STZ) (HY-13753)-induced diabetic mice. 7,4'-Dimethoxy-3-hydroxyflavone prevents thrombosis in mice without affecting bleeding time[1][2].
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SCH79797 dihydrochloride (Standard)
0 ImagesCat. No.: HY-14994RCAS No.: 1216720-69-2SCH79797 (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.
