Protease-activated Receptor

Vorapaxar (MK-5348) (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).

AY 77 (Unk-Cha-Chg-NH2) is a potent and selective PAR2 agonist. AY 77 showed selectivity for Ca2+ and ERK1/2 signaling (ec50 value of Ca2+ release was 40 nM and ec50 value of ERK1/2 phosphorylation was 2 μM). AY 77 can promote migration of human breast cancer cells in vitro.

BMS-986141(UDM-003183) is a selective and potent protease-activated receptor-4 (PAR-4) antagonist with oral activity and an IC50 value of 0.4 nM.BMS-98614 exhibits significant antithrombotic effects.

TRAP-6 (Thrombin Receptor Activator Peptide 6)(2TFA) is an agonist of protease-activated receptor 1 (PAR1).

Atopaxar (E5555), a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling. Atopaxar has been investigated for the treatment of Coronary Artery Disease and Acute Coronary Syndrome.

Trypsin is a serine protease that can be isolated from fish to hydrolyze lysine or arginine carboxy-side proteins. With the anti-inflammatory activity, Trypsin could induce the cell membrane fusion of PDCoV-infected cells through the interaction between the S glycoprotein of PDCoV and pAPN, activate PAR2 and PAR4, and promote cell proliferation and differentiation. Trypsin can be used to promote wound healing and study neurogenic inflammation.

Vorapaxar sulfate (Zontivity) is a potent and orally active thrombin receptor (PAR-1) antagonist.

Protease-Activated Receptor-2, amide (SLIGKV-NH2) is an agonist of PAR2 with an IC50 of 10.4 M.

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

ENMD-1068 HCl (ENMD 1068) is a PAR-2 antagonist. ENMD-1068 HCl inhibits the development of endometriosis in a mouse model.

tcY-NH2 TFA is a selective PAR4 antagonist peptide. Inhibits endostatin release and platelet aggregation induced by thrombin.

AZ3451 is an allosteric antagonist of protease-activated receptor-2 (PAR2, IC50: 23 nM).

SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is a PAR-2 agonist that induces non-histaminergic pruritus.

I-191 is a potent antagonist of protease-activated receptor 2 (PAR2), inhibits multiple signaling functions in human cancer cells.

Protease-Activated Receptor-1, PAR-1 Agonist acetate is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist acetate corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].

SCH79797 dihydrochloride is an effective and selective antagonist of protease activated receptor 1 (PAR1) with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects.

PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)), is a selective activator of the proteinase-activated receptor-4 (PAR-4) that does not affect PAR-1 or PAR-2, and its activity can be inhibited by a PAR-4 antagonist.

Thrombin Receptor Activator for Peptide 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).

LRGILS-NH2 acetate is a PAR-2-inactive reversed peptide.

2-Furoyl-LIGRLO-amide TFA(729589-58-6 free base) is a potent and selective protease-activated receptor 2 (PAR2) agonist.

FSLLRY-NH2 TFA is a is a protease-activated receptor 2 (PAR2) inhibitor. Reverses taxol-induced mechanical allodynia, heat hyperalgesia and PKC activation in ICR mice. Blocks ERK activation and collagen production in isolated cardiac fibroblasts. Also reduces symptoms in a mouse model of dermatophyte-associated itch.

SCH79797 is a potent and specific protease-activated receptor 1 (PAR1) antagonist with an IC50=70 nM with antimicrobial, anticancer, anti-inflammatory, and neuroprotective effects that attenuates thrombin-induced increase in CH25H expression in astrocytes, inhibits peritoneal dissemination of gastric cancer, and attenuates repetitive traumatic brain injury.

iso-TRAP-6 (iso-SFLLRN), a hexapeptide derived from the substitution of isoserine for serine, is a protease-activated receptor 1 (PAR1) agonist that activates platelets via PAR-1. iso-TRAP-6 is more resistant to degradation by plasma aminopeptidases than iso-TRAP-6.

Parmodulin 2 (ML 161) is the 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). It also inhibits thrombin-induced platelet activation.