protease activated receptor (par)

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].

Protease-Activated Receptor-1 (PAR-1) Agonist, a selective peptide, activates the PAR-1 receptor by mimicking the specific actions of thrombin. It corresponds to the PAR1 tethered ligand, facilitating selective activation of this receptor.

Protease-Activated Receptor-1 (PAR-1) Agonist TFA is a selective peptide that acts as an agonist for the proteinase-activated receptor-1 (PAR-1). Corresponding to the tethered ligand of PAR-1, this compound mimics the actions of thrombin through the PAR-1 receptor[1][2].

TFRGAP-amide, human PAR-3-derived tethered ligand sequence which does not activate PAR-3 but rather activates PAR-1 and PAR-2, either in Jurkat or in other PAR-expressing cells.

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA, is a peptide that acts as an agonist for the proteinase-activated receptor (PAR-3) [1].

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

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

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

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

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

TRAP-5 amide is a peptide agonist for protease-activated receptor 1 (PAR 1) [1].

PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide derived from protease-activated receptor 4 (PAR 4), serves as a specific agonist for PAR 4, exhibiting targeted activation properties.

SFNGGP-NH2 is a biologically active peptide that interacts with Protease-Activated Receptor 3 (PAR-3), a high-affinity thrombin receptor. Human cutaneous mast cells express PAR-3 mRNA, implicating a role in itch mechanotransduction, with both histamine-dependent and independent pathways reported. While PAR-3 alone does not induce itch, it may potentiate itch when co-expressed with PAR-4, enhancing thrombin's action. This suggests that PAR-3's primary function is not as a signal transmitter across the membrane, but rather as a cofactor necessary for PAR-4 activation.

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).

Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biologically active peptide functioning as a selective agonist for Protease Activated Receptor 1 (PAR-1) [a subtype of G-protein coupled receptors involved in mediating thrombin's cellular effects]. Exhibiting high specificity for PAR-1 over PAR-2, its selectivity was assessed via cell-based calcium signaling assays in HEK293 cells. As an agonist, it is instrumental for in vivo investigations of PAR-1 activation. PAR-1 also collaborates with PAR-4, influencing thrombin-induced hepatocellular carcinoma within [coagulation type] tumor environments where thrombin generation occurs.

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)

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

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.