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.

PAR related products

Structure Cat No. Product Name CAS No. Product Description
2-Furoyl-LIGRLO-amide 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.
2-Furoyl-LIGRLO-amide TFA 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.
AC 55541 V2850 AC 55541 916170-19-9 AC-55541 is anagonist of protease-activated receptor (PAR) 2.
Aeruginosin 98-B V71929 Aeruginosin 98-B 167228-01-5 Aeruginosin 98-B is a protease inhibitor.
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 V74510 Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 211190-38-4 Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biologically active peptide.
Atopaxar V6725 Atopaxar 751475-53-3 Atopaxar, formerly known as E5555, is a potent and orally -active PAR-1 inhibitor.
AY254 V74516 AY254 2093408-03-6 AY254 is an analogue of AY77.
AY77 V74515 AY77 1835734-92-3 AY77 is a calcium-biased PAR2 agonist.
AZ3451 V31712 AZ3451 2100284-59-9 AZ3451 is a protease-activated receptor-2 (PAR2) antagonist (inhibitor) with IC50 of 23 nM.
BMS-986120 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.
CL-417513 V51013 CL-417513 313986-65-1 PAR2 inhibitor
FR-171113 V74514 FR-171113 173904-50-2 FR171113 is a specific non-peptide thrombin receptor antagonist.
FSLLRY-NH2 V74501 FSLLRY-NH2 245329-02-6 FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
FSLLRY-NH2 TFA V76998 FSLLRY-NH2 TFA FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
GB-110 hydrochloride V76986 GB-110 hydrochloride GB-110 HCl is a potent, orally bioactive, non-peptide protease activated receptor 2 (PAR2) agonist.
I-191 V25156 I-191 1690172-25-8 I-191 is a potent antagonist of protease-activated receptor 2 (PAR2).
I-287 V69828 I-287 2014368-93-3 I-287 is an orally bioactive and selective inhibitor of PAR2 that negatively regulates Gαq and Gα12/13 activities and their downstream effectors.
ML161 (Parmodulin 2) V2419 ML161 (Parmodulin 2) 423735-93-7 ML-161 is a novel and potent allosteric inhibitor of PAR1 (proteinase-activated receptor 1) on platelets with IC50 of 0.26 μM.
P4pal10 V74512 P4pal10 1021346-05-3 P4pal10 is a PAR4 antagonist.
PAR 4 (1-6) (TFA) (GYPGQV TFA) V81041 PAR 4 (1-6) (TFA) (GYPGQV TFA) PAR 4 (1-6) TFA (GYPGQV TFA) is a hexapeptide that is a fragment of protease-activated receptor 4 (PAR4) and works as a specific inhibitor of PAR4.
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