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 (4)
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Protease Activated Receptor (PAR) Isoform Comparison
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TFLLRN-NH2
0 ImagesTFLLRN-NH2 is a biological active peptide. (PAR-1 Agonist)
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RWJ-56110 dihydrochloride
0 ImagesRWJ-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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Protease-Activated Receptor-4
0 ImagesCat. No.: HY-P0297CAS No.: 245443-52-1Protease-Activated Receptor-4 is the agonist of proteinase-activated receptor-4 (PAR4).
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ML354
0 ImagesSynonyms: VU0099704ML354 is a selective PAR4 antagonist with an IC50 of 140 nM.
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VKGILS-NH2
0 ImagesVKGILS-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.
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FSLLRY-NH2 TFA
0 ImagesCat. No.: HY-P1260APurity: 98.97%FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
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Cathepsin G
0 ImagesCat. No.: HY-P3012CAS No.: 107200-92-0Cathepsin G is a pH-dependent serine protease. Cathepsin G hydrolyzes diverse synthetic and protein substrates and remodels extracellular matrix. Cathepsin G exerts immunomodulatory effects via recruiting phagocytes, enhancing T cell motility, activating ERK1/2 and p38 MAPK signaling, and mediating PKCζ membrane translocation. Cathepsin G regulates inflammatory responses by cleaving inflammatory mediators. Cathepsin G participates in vascular regulation by converting angiotensin I to angiotensin II. Cathepsin G induces PAR4-dependent platelet activation, facilitates platelet-neutrophil aggregation, and mediates VITT-related NETosis, thrombus formation. Cathepsin G can be used for the research of immune thrombotic thrombocytopenia, cardiovascular disease, and select autoimmune and inflammatory diseases.
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PAR-4 (1-6) amide (human)
0 ImagesPAR-4 (1-6) amide human is an N-terminal fragment of protease-activated receptor 4 (PAR4). PAR-4 (1-6) amide human induce platelet aggregation.
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P4pal10 TFA
0 ImagesCat. No.: HY-P5875APurity: 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.
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iso-TRAP-6
0 ImagesSynonyms: iso-SFLLRN
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CBK289001
0 ImagesCBK289001 is a tartrate-resistant acid phosphatase (TRAP/ACP5) inhibitor. CBK289001 inhibits TRAP 5bMV, TRAP 5bOX and TRAP 5aOX with IC50s of 125 µM, 4.21 µM and 14.2 µM, respectively.
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FLLRN
0 ImagesSynonyms: TRAP-6 (2-6)FLLRN is a biological active peptide. (PAR1-specific antagonist peptide)
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Murine Thrombin
0 ImagesCat. No.: HY-114164GCAS No.: 9002-04-4Murine Thrombin is a murine serine protease that plays a central role in blood coagulation. Murine Thrombin stimulates macrophages to polarize into a unique phenotype characterized by anti-inflammatory and pro-repair properties. Murine Thrombin activates PAR1, induces the production of MCP-1, MMP3 and VEGF in mouse intervertebral discs, and causes degradation of the cartilage matrix and destruction of intervertebral disc structure. Murine Thrombin activity increases significantly in paraoxon-induced status epilepticus.
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PAR4 antagonist 6
0 ImagesCat. No.: HY-159632Purity: 99.35%PAR4 antagonist 6 (Compound 12) is a PAR4 antagonist, with IC50 values of 134 and 401 nM for hPAR4 (PAC1) and mPAR4 (PAC1), respectively.
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Activated protein C
0 ImagesCat. No.: HY-P2933CAS No.: 42617-41-4Activated protein C is an anticoagulant targeting coagulation factors Va and VIIIa. Activated protein C demonstrates cytoprotective effects through binding to endothelial cell protein C receptor (EPCR) and protease-activated receptor-1 (PAR-1), regulating gene expression, anti-inflammation, anti-apoptosis, and stabilizing endothelial barriers. Activated protein C is promising for research of diseases such as severe sepsis and ischemic stroke.
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PAR2 modulator-1
0 ImagesPAR2 modulator-1 is a biased protease-activated receptor 2 (PAR2) inhibitor. PAR2 modulator-1 blocks the PAR2-dependent MAPK signaling pathway with an IC50 value of 8.5 μM, without altering the PAR2-dependent Ca2+ signaling pathway. PAR2 modulator-1 blocks pain responses induced by PAR2 agonists. PAR2 modulator-1 can be used in the research of chronic pain.
