AC264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). Displays no activity at other PAR subtypes and exhibits no significant activity at over 30 other receptors implicated in nociception and inflammation.

AZ3451 is a potent and selective allosteric antagonist of protease-activated receptor 2 (PAR2)

AZ-8838 (AZ8838) is a potent, and selective PAR2 antagonist with Kd of 125 nM.

BMS-986120 (BMS986120) is a potent, selective, orally bioavailable, and reversible PAR4 antagonist with Kd of 0.098 nM for human PAR4.

E5555 shows potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC values of 0.064 and 0.031 μM respectively.

GB-110 is a potent, non-peptidic agonist of PAR2 that selectively induces PAR2-mediated intracellular Ca(2+) release in HT29 cells with EC50 of 0.28 uM.

GB-88 is a selective, orally available PAR2 antagonist that inhibits PAR2 activated Ca(2+) release with IC50 of 2 uM.

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). Thought to act allosterically. Also inhibits thrombin-induced platelet activation.

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

PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects.

RWJ-56110 dihydrochloride 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 dihydrochloride 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. RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.

FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.

FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.

tcY-NH2 is a selective rat PAR4 antagonist peptide. tcY-NH2 inhibits thrombin- and AY-NH2-induced rat platelet aggregation.

tcY-NH2 TFA is a selective rat PAR4 antagonist peptide. tcY-NH2 TFA inhibits thrombin- and AY-NH2-induced rat platelet aggregation.

SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) is an agonist of Protease-Activated Receptor-2 (PAR-2).

PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is a fragment of protease-activated receptor 4 (PAR4) and acts as PAR4-specific agonist.

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

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

Protease-Activated Receptor-1, PAR-1 Agonist is a thrombin-specific, protease-activated receptor 1 (PAR-1)-specific agonist peptide.

Protease-Activated Receptor-3 (PAR-3) (1-6), human is a proteinase-activated receptor (PAR-3) agonist peptide.

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a proteinase-activated receptor (PAR-3) agonist peptide.