Protease-Activated Receptors (PAR)

BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively.

Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.

AC-264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5).

ML-161 is an inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets).

Thrombin Receptor Activator for Peptide 5 (TRAP-5), coagulation factor II (thrombin) receptor is a G protein-coupled receptor involved in the regulation of thrombotic response.

I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.

GB110 is a Novel potent non-peptide PAR2 agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.

GB-88 is a novel selective, orally available PAR2 antagonist, inhibits PAR2 activated Ca2+ release with an IC50 of 2 ?M.

UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM).

AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.

AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation.

TRAP-6 amide is a PAR-1 thrombin receptor agonist peptide.

Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor.

PAR-2 (1-6) (human) (SLIGKV), a peptide ligand, is a PAR-2 agonist.

iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. iso-TRAP-6 is an analog of TRAP-6 that refers to the use of isoserine instead of serine as first amino acid.

FLLRN is a biological active peptide. (PAR1-specific antagonist peptide)

AY254 is an analogue of AY77. AY254 is ERK-biased PAR2 agonist with an EC50 of 2 nM. AY254 relieves cytokine-induced caspase 3/8 activation. AY254 also promotes scratch-wound healing and induced IL-8 secretion via PAR2-ERK1/2 signaling.

AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release.