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.

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.

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

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

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

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

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

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

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.

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

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].

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

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).

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.

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.

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.

Protease-Activated Receptor-4 diTFA,2454 is the proteinase-activated receptor-4 (PAR4)agonist

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.

ML-354 (VU0099704) is a selective and potent PAR4 antagonist for the study of cardiovascular disease.

PAR-4 Agonist Peptide, amide (AY-NH2), is an agonist of proteinase-activated receptor-4 (PAR-4).

VKGILS-NH2 Acetate is a reversed amino acid sequence control peptide for SLIGKV-NH2, a protease-activated receptor 2 (PAR2) agonist.

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.

PAR-2-IN-1 (IUN76750) is a PAR- 2 signaling pathway inhibitor with anti-inflammatory and anticancer effects.

TFLLR-NH2 2TFA(197794-83-5(free base)) is an agonist of PAR1 (EC50 :1.9 μM).

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.

AC-55541 (AOB2796) is a novel 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.

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

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.

Atopaxar, 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.

Protease-Activated Receptor-4 (PAR4) is a proteinase-activated receptor-4 agonist used in antiplatelet therapy.

Thrombin Receptor Activator for Peptide 5 (TRAP-5), also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is utilized in coronary heart disease (CHD) research.

TFLLR-NH2(2TFA) is an agonist of PAR1 (EC50 :1.9 μM).

PAR650097 is a humanized monoclonal antibody targeting PAR2, used in migraine research.

PAR-4 Agonist Peptide, amide acetate is an agonist of proteinase-activated receptor-4 (PAR-4).

AC-264613 is an agonist of the GPCR protease-activated receptor 2 (PAR2). AC-264613(AC264613) suppresses interferon regulatory factor 5 and decreases interleukin-12p40 production by lipopolysaccharide-stimulated macrophages. AC-264613(AC264613) activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 30 to 100 nM.