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].

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.

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.

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.

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

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

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.

Vorapaxar (MK-5348) is a selective, orally active, and competitive antagonist of the plasminogen activator receptor (PAR-1) with a Ki value of 8.1 nM. Vorapaxar primarily acts by targeting PAR-1 on the platelet surface to block thrombin-induced platelet activation. Vorapaxar is suitable for use in cardiovascular disease research.

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

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

H-Ser-Phe-Leu-Leu-Arg-OH, also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is utilized in coronary heart disease (CHD) research.

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

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

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

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

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

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

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].

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].

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.

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.

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.

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.