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 (142)
Related Products (142)
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Recombinant Proteins (4)
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Protease Activated Receptor (PAR) Isoform Comparison
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TFMU-ADPr diammonium
0 ImagesCat. No.: HY-146248BPurity: 98.78%TFMU-ADPr diammonium is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr diammonium can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr diammonium binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr diammonium can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr diammonium is also applicable to COVID-19-related research.
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PZ-128
0 ImagesSynonyms: P1pal-7PZ-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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I-287
0 ImagesI-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.
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PAR-4 Agonist Peptide, amide TFA
0 ImagesSynonyms: PAR-4-AP TFA; AY-NH2 TFAPAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist.
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PAR-2 (1-6) (human)
0 ImagesPAR-2 (1-6) (human) (SLIGKV), a peptide ligand, is a PAR-2 agonist.
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GB-110 hydrochloride
0 ImagesCat. No.: HY-120528APurity: 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.
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Atopaxar
0 ImagesSynonyms: E5555; ER-172594-00Atopaxar (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.
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PPACK dihydrochloride
0 ImagesSynonyms: Pebac; D-Phenylalanyl-prolyl-arginyl Chloromethyl Ketone; D-Phe-Pro-Arg-CH2ClPPACK dihydrochloride is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK dihydrochloride specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK dihydrochloride exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK dihydrochloride binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK dihydrochloride is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.
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AC-55541
0 ImagesAC-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.
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ENMD-1068 hydrochloride
0 ImagesENMD-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.
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Vorapaxar sulfate
0 ImagesSynonyms: SCH 530348 sulfateVorapaxar 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.
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TRAP-7
0 ImagesTRAP-7 is a thrombin receptor (PAR) activating peptide. TRAP-7 stimulates total inositol phosphate (IP) accumulation and phosphorylation of a specific endogenous substrate for activated PKC. TRAP-7 can be used in cardiovascular disease research.
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SCH79797 dihydrochloride
0 ImagesSCH79797 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.
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AC-264613
0 ImagesAC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC50 of 7.5.
