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.The PAR family consists of four members: PAR1, PAR2, PAR3, and PAR4. PARs are significant targets for pharmaceuticals and have vital roles in the vasculature, inflammation, and cancer.
With the exception of red blood cells, PARs are expressed on almost all blood and blood vessel wall cell types (ECs, fibroblasts, myocytes), as well as on platelets, neutrophils, macrophages, and leukemic white blood cells. Immune cells, astrocytes, neurons, and epithelium all express thrombin-activated PAR-1, PAR-3, and PAR-4. Human vascular, intestinal, neuronal, and airway cells contain PAR-2, which is activated by serine proteases similar to trypsin. Its expression rises in tissues that have been injured or in response to inflammatory mediator stimulation.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V74503 | PAR-2 (1-6) (human) | 202933-49-1 | PAR-2 (1-6) (human) (SLIGKV) is a bioactive peptide agonist of PAR-2. |
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V2173 | PAR-2 inhibitor | 1690176-75-0 | PAR-2-IN-1 is a protease-activated receptor 2 (PAR2) signaling pathway inhibitor (antagonist) with anti~inflammatory and anti-cancer effects. |
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V81048 | Parstatin (human) TFA | Parstatin (human) TFA is a cell-permeable (penetrable) peptide agonist of the PAR-1 thrombin receptor and a potent angiogenesis inhibitor. | |
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V51033 | Parstatin (mouse) | 1065756-01-5 | Parstatin(mouse) is a cell-penetrating/penetrable peptide agonist of the PAR-1 thrombin receptor and a potent angiogenesis inhibitor. |
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V74507 | Parstatin(human) | 1065755-99-8 | Parstatin (human) is a cell-penetrating/penetrable peptide agonist of the PAR-1 thrombin receptor and a potent angiogenesis inhibitor. |
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V76657 | Parstatin(mouse) TFA | Parstatin(mouse) TFA is a cell-penetrating/penetrable peptide agonist of the PAR-1 thrombin receptor and a potent angiogenesis inhibitor. | |
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V76616 | pNP-ADPr disodium (ADP-ribose-pNP disodium) | pNP-ADPr disodium is a colorimetric substrate for the continuous determination of the activity of Poly(ADP-ribose) glycohydrolase (PARG) and ADP-ribosyl hydrolase 3 (ARH3). | |
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V74513 | Protease-Activated Receptor-1, PAR-1 Agonist | 141136-85-8 | Protease-Activated Receptor-1, PAR-1 Agonist is a selective protease-activated receptor 1 (PAR-1) agonist peptide. |
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V76590 | Protease-Activated Receptor-1, PAR-1 Agonist TFA | Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective protease-activated receptor 1 (PAR-1) agonist peptide. | |
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V32060 | Protease-Activated Receptor-2, amide (SLIGKV-NH2) | 190383-13-2 | Protease-Activated Receptor-2, amide (peptide sequence shortening: SLIGKV-NH2), an activating peptide of PAR2, is a novel, highly potent and selective agonist of protease-activated receptor-2 (PAR2) (Ki = 9.64 μM; IC50 = 10.4 μM). |
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V74517 | Protease-Activated Receptor-3 (PAR-3) (1-6), human | 1872435-09-0 | Protease-Activated Receptor-3 (PAR-3) (1-6), human is a protease-activated receptor 3 (PAR-3) agonist peptide. |
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V76589 | Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA | Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a protease-activated receptor 3 (PAR-3) agonist peptide. | |
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V74508 | Q94 hydrochloride | 1052076-77-3 | Q94 hydrochlo is a selective PAR1 antagonist (IC50=916 nM) that can selectively block PAR1/Gαq interaction and signaling. |
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V74506 | SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) | 2828432-39-7 | SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) is a protease-activated receptor-2 (PAR-2) agonist. |
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V74511 | tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) | 327177-34-4 | tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) is a potent PAR4-selective peptide antagonist. |
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V74502 | tcY-NH2 TFA ((trans-Cinnamoyl)-YPGKF-NH2 TFA) | 1262750-73-1 | tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) TFA is a potent PAR4-selective peptide antagonist. |
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V74498 | TFLLRN-NH2 | 244095-36-1 | TFLLRN-NH2 is a biologically active peptide. |
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V81564 | TFMU-ADPr triethylamine | TFMU-ADPr triethylamine is a extensively usedsubstrate for monitoring polyATP-ribose hydrolase (PARG) activity. | |
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V74509 | TRAP-6 amide TFA | 1426807-16-0 | TRAP-6 amide TFA is a bioactive peptide agonist of the PAR-1 thrombin receptor. |
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V74500 | VKGILS-NH2 | 942413-05-0 | VKGILS-NH2 is a reverse amino acid (AA) sequence control peptide of SLIGKV-NH2, an agonist of protease-activated receptor 2 (PAR2), which has no effect on DNA synthesis in cells. |
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