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 |
|---|---|---|---|---|
|
V112324 | (R)-AZ8838 | 2151021-59-7 | (R)-AZ8838 is a competitive PAR2 antagonist with a pKi value of 5.2 for human PAR2. |
|
V122002 | (Rac)-AZ8838 | 2100283-63-2 | (Rac)-AZ8838 is a conformational antagonist of protease-activated receptor 2 (PAR2) and can be used to study pain and inflammation-related diseases. |
|
V123612 | 1-Methyladenosine-d3 | 1-Methyladenosine-d3 is a deuterium-labeled 1-methyladenosine. | |
|
V123232 | 15-Deoxy-Δ12,14-Prostaglandin J2-2-glyceryl ester | 1947405-90-4 | 15-Deoxy-Δ12,14-Prostaglandin J2-2-glyceryl ester is a derivative of 15-deoxy-Δ-12,14-prostaglandin J2. |
|
V123253 | 15-LOX-IN-2 | 15-LOX-IN-2 is an orally effective COX-2/15-LOX inhibitor and a partial agonist of PPARγ. | |
|
V74499 | 2-Furoyl-LIGRLO-amide | 729589-58-6 | 2-Furoyl-LIGRLO-amide is a potent and specific protease-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0. |
|
V74504 | 2-Furoyl-LIGRLO-amide TFA | 2468029-34-5 | 2-Furoyl-LIGRLO-amide TFA is a potent and specific protease-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0. |
|
V126937 | 5-cis Carbaprostacyclin | 69609-77-4 | 5-cis Carbaprostacyclin is a PGI2-stable analog based on carbaprostacyclin. |
|
V128046 | ABP/PPAR modulator 1 | 3104894-76-7 | ABP/PPAR modulator 1 is an orally effective multimodal regulator of FABP and PPAR (IC50 for FABP1 and FABP4 are 0.65 μM and 1.08 μM, respectively, and EC50 for PPARα, PPARγ and PPARδ are 9.19 μM, 2.20 μM and 1.58 μM, respectively). |
|
V2850 | AC 55541 | 916170-19-9 | AC-55541 is anagonist of protease-activated receptor (PAR) 2. |
|
V71929 | Aeruginosin 98-B | 167228-01-5 | Aeruginosin 98-B is a protease inhibitor. |
|
V74510 | Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 | 211190-38-4 | Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biologically active peptide. |
|
V118411 | Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 TFA | Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 TFA is a bioactive peptide and a selective protease receptor 1 (PAR-1) agonist, with higher specificity for PAR-1 than for PAR-2. | |
|
V74516 | AY254 | 2093408-03-6 | AY254 is an analogue of AY77. |
|
V74515 | AY77 | 1835734-92-3 | AY77 is a calcium-biased PAR2 agonist. |
|
V31712 | AZ3451 | 2100284-59-9 | AZ3451 is a protease-activated receptor-2 (PAR2) antagonist (inhibitor) with IC50 of 23 nM. |
|
V3483 | BMS-986120 | 1478712-37-6 | BMS-986120 (BMS986120) is a novel, potent and orally bioactive antagonist of protease-activated receptor-4 (PAR4) with the potential to be used forthrombus propagation and pathological vascular occlusion. |
|
V51013 | CL-417513 | 313986-65-1 | PAR2 inhibitor |
|
V132506 | CS4 | CS4 is a selective HDAC inhibitor with IC50 values of 38 nM, 12 nM, 5.8 μM, 19 μM, and 61 μM for HDAC1, HDAC6, HDAC8, HDAC4, and HDAC11, respectively. | |
|
V132549 | CUDA disodium | CUDA disodium is a potent soluble epoxide hydrolase (sEH) inhibitor with IC50 values of 11.1 nM for mouse sEH and 112 nM for human sEH. |