par 2

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

PAR2 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of mouse and rat PAR2. It also corresponds to residues 39-44 and 37-42 of the mouse and rat full-length sequences, respectively. PAR2 (1-6) induces relaxation in precontracted rat arteries in a concentration-dependent manner, an effect that can be reduced by the nitric oxide synthase inhibitor L-NNA . It inhibits keratinocyte growth in the presence and absence of growth factors. PAR2 (1-6) inhibits LPS-induced pulmonary neutrophil influx and increases in matrix metalloproteinase-2 (MMP-2) activity in mice.

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

PAR2modulator-1 (Compound C781) is an antagonist of the protease-activated receptor 2 (PAR2). It specifically inhibits the PAR2-dependent MAPK signaling pathway with an IC50 value of 8.5 μM. PAR2modulator-1 can effectively block pain responses triggered by PAR2 agonists. This compound is useful for research in inflammation, immunology, and neurological disorders, including chronic pain and asthma.

Anti-PAR2 Antibody is a neutralizing monoclonal antibody targeting Protease-activated Receptor 2 (PAR2). By specifically binding to its extracellular domain and interfering with protease-mediated receptor activation, this antibody effectively inhibits downstream inflammatory signaling and nociceptive transmission, and is commonly used in studies of acute/chronic inflammation, neurogenic pain, and dermatological conditions.

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.

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.

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

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

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

GB-88 is an orally active, highly selective, non-peptide PAR2 antagonist that blocks downstream inflammatory and pain signaling pathways by inhibiting PAR2-mediated Ca²⁺ release (IC₅₀ = 2 μM). GB-88 exhibits antagonistic activity against various PAR2 agonists, including trypsin, SLIGRL-NH₂, and GB110, and shows no significant cross-reactivity with PAR1, PAR3, or PAR4. GB-88 is suitable for research into diseases such as inflammation, pain, and metabolic disorders.

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

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.

PAR-2-IN-2 (compound P-596) is an inhibitor of protease-activated receptor 2 (PAR-2), with an IC50 of 10.79 μM for SLIGKV and an IC50 greater than 200 μM for trypsin.

PAR-2 (1-6) (human) (SLIGKV), a peptide ligand and PAR-2 agonist, [1].

PAR-2 antagonist 1 (Compound 9a) is a protease-activated receptor 2 (PAR2) antagonist with an IC50 of 0.9 μM. It effectively inhibits the proliferation and migration of breast cancer cells.

Prostate apoptosis response protein PAR-4 (2-7) [Homo sapiens] is a peptide with the sequence H2N-Ala-Thr-Gly-Gly-Tyr-Arg-OH, MW= 623.66.

PAR4 antagonist 2 (Compound 31) is a protease-activated receptor 4 (PAR4) antagonist with IC50 values of 95 nM for human PAR4 and 367 nM for mouse PAR4. It inhibits the activation of PAR4 through cleavage by the natural protease thrombin but has no effect on the synthetic PAR4 agonist peptide AYPGKF.

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

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

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.

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

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