iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. iso-TRAP-6 is an analog of TRAP-6 (HY-P0078) that refers to the use of isoserine instead of serine as first amino acid[1].
Parstatin(mouse), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis[1][2].
CBK289001 (CBK-289001) is a small molecule inhibitor of Tartrate-resistant acid phosphatase (TRAP/ACP5), demonstrates efficacy in a migration assay and IC50 values from 4 to 125 uM.
Parmodulin 2 (ML161),a probe, is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 inhibits platelet aggregation induced by a PAR1 peptide agonist or by thrombin and has shown cytoprotective effects[1, 2].
RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 blocks angiogenesis and blocks the formation of new vessel in vivo. RWJ-56110 induces cell apoptosis[1][2].
Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.
GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM[1].
TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.
FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM.[1][2][3][4].
tcY-NH2 is a selective rat PAR4 antagonist peptide. tcY-NH2 inhibits thrombin- and AY-NH2-induced rat platelet aggregation[1][2].
ML354 is a selective PAR4 antagonist with an IC50 of 140 nM[1].
TRAP-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[1].
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 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 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes[1][2][3][4].
Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease[1][2].
TRAP-6-IN-1 (Compound 8) is a dual collagen and TRAP-6 inhibitor with IC50 values of 17.12 µM and 11.88 µM against collagen and TRAP-6, respectively. TRAP-6-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner[1].
BMS-986120 is an antagonist of the Platelet Protease-Activated Receptor-4 (PAR4), with IC50s of 9.5, 2.1 nM in human and monkey blood, respectively.
YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC50 of 7.5[1].
AY 254 is a potent PAR2 biased agonist. Selectively activates ERK1/2 signaling (EC50= 2 nM for ERK1/2 phosphorylation versus 80 nM for Ca2+release). Reduces cytoKi ne-induced caspase 3/8 activation, promotes scratch-wound healing, and induces IL-8 secretion, in human colorectal cancer (HT29) cellsin vitro.
Aeruginosin 98-B is a protease inhibitor. Aeruginosin 98-B inhibits trypsin, plasmin and thrombin with IC50 values of 0.6, 7.0 and 10.0 μg/mL, respectively[1].
GB83 is a potent PAR2 antagonist. GB83 reverses neutrophil elastase‐induced synovitis and pain. GB83 blocks the effect of MET-1 supernatant on NG neurons[1].
PAR-2 (1-6) (human) (SLIGKV), a peptide ligand, is a PAR-2 agonist[1].
Protease-Activated Receptor-4 is the agonist of proteinase-activated receptor-4 (PAR4).
AC-55541 is a novel small-molecule protease-activated receptor 2(PAR2) agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM.IC50 value: 200-1000 nM(EC50) [1]Target: PAR2 agonistNeither AC-55541 nor AC-264613 had activity at any of the other PAR receptor subtypes, nor did they have any significant affinity for over 30 other molecular targets involved in nociception. Visualization of EYFP-tagged PAR2 receptors showed that each compound stimulated internalization of PAR2 receptors. AC-55541 was well absorbed when administered intraperitoneally to rats, reaching micromolar peak plasma concentrations. AC-55541 was stable to metabolism by liver microsomes and maintained sustained exposure in rats, with elimination half-lives of 6.1 h. Intrapaw administration of AC-55541 or AC-264613 elicited robust and persistent thermal hyperalgesia and edema. Coadministration of either a tachykinin 1 (neurokinin 1) receptor antagonist or a transient receptor potential vanilloid (TRPV) 1 antagonist completely blocked these effects. Systemic administration of either AC-55541 or AC-264613 produced a similar degree of hyperalgesia as was observed when the compounds were administered locally.
SFNGGP-NH2 is a biological active peptide. (PAR-3 is a high-affinity thrombin receptor. PAR-3 mRNA is expressed in the cutaneous mast cells of humans. Protease-Activated Receptors (PARs) have been studied for their roles in itch and their itch-associated response through histamine-dependent/independent pathways have been reported. PAR-3 has been shown not to induce itching alone but possibly in conjunction with PAR-4. Co-expression of PAR-3 and PAR-4 enhances thrombin action suggesting that PAR-3 alone does not mediate transmembrane signaling but instead functions as a cofactor to activate PAR-4.)
TRAP-5 amide is a protease-activated receptor 1 (PAR 1) agonist peptide[1].
TRAP-6 amide is a PAR-1 thrombin receptor agonist peptide[1].
Thrombin Receptor Activator for Peptide 5 (TRAP-5) is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD).