par-4

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.

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.

PAR-4 (1-6) amide human, an N-terminal fragment of protease-activated receptor 4 (PAR4), induces platelet aggregation [1].

PAR-4 (1-6), mouse is a polypeptide molecule with the sequence GYPGKF.

UDM-001651 is an effective and orally bioavailable protease-activated receptor 4 antagonists (IC50=4 nM; Kd=1.4 nM). UDM-001651 displays antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay.

BMS-986120 is a first-in-class oral, reversible protease-activated receptor 4 (PAR4) antagonist with IC50s of 9.5 nM in human blood and 2.1 nM in monkey blood, exhibiting potent and selective antiplatelet effects[1][2].

Compound 12, a PAR4 antagonist6, exhibits inhibitory activity with IC50 values of 134 nM and 150 nM against hPAR4 and mPAR4, respectively.

PAR4 antagonist3 (Compound 36) is a selective antagonist of protease-activated receptor 4 (PAR4). It exhibits antiplatelet activity with an IC50 of 26.1 nM and enhances metabolic stability in human liver microsomes, with a half-life (T1/2) of 97.6 minutes.

PAR4 antagonist4 (Compound 37) is a selective antagonist of protease-activated receptor 4 (PAR4). It exhibits antiplatelet activity with an IC50 of 14.2 nM. Moreover, PAR4 antagonist3 enhances metabolic stability in human liver microsomes, showing a half-life (T1/2) of 42.5 minutes.

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.

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

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.

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.

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

PAR 4 (1-6) can be used for relevant research in the life sciences. Its product number is T36293 and CAS number is 225779-44-2.

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.

PAR4 antagonist7 (Compound 20f) is a selective PAR4 antagonist (IC50: 1.72 nM), effective in inhibiting platelet aggregation induced by PAR4 agonists. It exhibits good metabolic stability and has not shown any tendency to cause bleeding in mice.

PAR4 antagonist8 (Compound 20f) is an effective oral and selective PAR4 antagonist with an IC50 of 15.32 nM, boasting favorable pharmacokinetic properties. It effectively inhibits human platelet aggregation induced by PAR4 agonists (IC50=6.39 nM) and also suppresses platelet aggregation in mice. PAR4 antagonist8 is utilized in anti-thrombotic research.

PAR4 antagonist 5 (compound 1), a potent PAR4 antagonist, exhibits anti-platelet aggregation activity with an IC50 of less than 20 μM. This compound is useful for thrombosis disease research [1].

Arylquin 1, a prostate-apoptosis-response-4 (Par-4) secretagogue, specifically targets vimentin to facilitate Par-4 secretion. It also induces lysosomal membrane permeabilization (LMP) and promotes non-apoptotic cell death in cancer cells [1].

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)

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 μM), showing no effect on PAR-2, PAR-3, or PAR-4. It inhibits the aggregation of human platelets induced by SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), with high selectivity relative to U46619. RWJ-56110 dihydrochloride also blocks angiogenesis and the formation of new vessels in vivo, and induces cell apoptosis[1][2].

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