Home > Inhibitors & Agonists > GPCR > Protease-activated Receptor (PAR)
Cat. No. Product name CAS No.
DC10117 AC264613 Featured

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.

1051487-82-1
DC10879 AZ3451 Featured

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

2100284-59-9
DC11742 AZ-8838

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

2100285-41-2
DC11923 BMS-986120

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

1478712-37-6
DC8533 E5555 hydrobromide

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.

474550-69-1
DC11741 GB-110

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.

1252806-70-4
DC11740 GB-88

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

1416435-96-5
DC7197 ML 161 Featured

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.

423735-93-7
DC8860 Vorapaxar Featured

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

618385-01-6
DC40079 PZ-128

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.

371131-16-7
DC40104 RWJ-56110 dihydrochloride

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 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.

2387505-58-8
DC40332 ENMD-1068 hydrochloride

ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist with antiangiogenic and anti-inflammatory activities. ENMD-1068 hydrochloride reduces epatic stellate cells (HSCs) activation and collagen expression through the inhibiton of TGF-β1/Smad signal transduction.

DC41699 FSLLRY-NH2

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

DC41700 FSLLRY-NH2 TFA

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

DC41701 tcY-NH2

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

327177-34-4
DC41702 tcY-NH2 TFA

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

DC41755 SLIGRL-NH2 TFA

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

DC41761 PAR 4 (1-6) (TFA)

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

DC41909 TRAP-6 amide

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

141923-40-2
DC41910 TRAP-6 amide TFA

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

1426807-16-0
DC42020 Protease-Activated Receptor-1, PAR-1 Agonist

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

141136-85-8
DC42021 Protease-Activated Receptor-3 (PAR-3) (1-6), human

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

1872435-09-0
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