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 |
|---|---|---|---|---|
|
V74505 | VKGILS-NH2 TFA | 2828432-41-1 | VKGILS-NH2 TFA 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. |
|
V4229 | Vorapaxar | 618385-01-6 | Vorapaxar (formerly SCH-530348; SCH530348; Zontivity), a new anti-platelet drug based on the natural product himbacine, is a thrombin receptor protease-activated receptor (PAR-1) antagonist that inhibits thrombin-induced platelet activation. |
|
V4230 | Vorapaxar sulfate | 705260-08-8 | Vorapaxar sulfate, the sulfuric acid salt form of Vorapaxar (also known as SCH-530348; Zontivity), is an orally bioactive anti-platelet drug acting as a thrombin receptor protease-activated receptor (PAR-1) antagonist. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
