Protease-Activated Receptors (PAR)

PAR4 antagonist 3 is a selective inhibitor of protease-activated receptor 4 (PAR4). This compound demonstrates significant antiplatelet activity, with an IC50 value of 26.1 nM, making it a valuable tool for studies related to thrombosis and platelet function. Additionally, PAR4 antagonist 3 shows improved metabolic stability in human liver microsomes, with a half-life of 97.6 minutes, enhancing its potential for in vivo applications.

Q94 hydrochloride is a selective antagonist of the protease-activated receptor 1 (PAR1), with an IC50 value of 916 nM. It inhibits PAR1/Gαq interaction and signaling, effectively preventing PAR1-mediated increases in CCL2 mRNA and protein levels in a dose-dependent manner. Additionally, Q94 hydrochloride completely blocks thrombin-induced phosphorylation of ERK1/2 and MLC, making it a valuable tool for investigating PAR1-related pathways in various biological research applications.

Protease-Activated Receptor-1 Antagonist 2 is a potent oral antagonist of the protease-activated receptor-1 (PAR-1), exhibiting an IC50 value of 7 nM. This compound demonstrates favorable pharmacokinetic properties, making it an essential tool for studying cardiovascular diseases, including atherosclerosis and restenosis. Its targeted action on PAR-1 allows for in-depth exploration of its role in vascular biology and potential therapeutic interventions.

2-Furoyl-LIGRLO-amide TFA is a selective agonist for the proteinase-activated receptor 2 (PAR2), demonstrating a pD2 value of 7.0. This compound is utilized in biochemical research to study PAR2 signaling pathways and their role in various physiological processes, including inflammation and pain modulation. Its potency and selectivity make it a valuable tool for investigating the therapeutic potential of targeting PAR2 in disease models.

VKGILS-NH2 TFA is a reversed amino acid sequence control peptide targeting protease-activated receptor 2 (PAR2). This compound serves as a PAR agonist and is utilized in research to delineate receptor activity and signal transduction pathways. VKGILS-NH2 TFA exhibits no impact on DNA synthesis in cells, making it a suitable control for studies involving PAR2 activation.

(R)-AZ8838 is a competitive antagonist of the human PAR2 (protease-activated receptor 2) with a pKi value of 5.2. This compound demonstrates anti-inflammatory effects, evidenced in a rat model of PAR2 agonist-induced paw edema. It is valuable for research applications focusing on inflammation, pain modulation, and receptor signaling pathways.

BAY-386 is a potent Protease Activated Receptor-1 (PAR-1) antagonist that effectively inhibits the expression of pro-inflammatory factors such as MCP-1 and CXCL1 in human umbilical vein endothelial cells (HUVEC). This compound is valuable for research into inflammatory processes and vascular biology, providing insights into PAR-1 signaling pathways and their role in inflammation-related conditions.

ENMD-1068 hydrobromide is a potent antagonist of the proteinase-activated receptor 2 (PAR2). It effectively attenuates joint inflammation in a dose-dependent manner, making it a valuable tool for investigating inflammatory pathways. This compound is primarily utilized in research related to joint inflammation and therapeutic approaches targeting PAR2.

P4pal10 is a potent antagonist of the protease-activated receptor 4 (PAR4). It effectively inhibits platelet aggregation and tissue factor (TF)-induced thrombin generation, exhibiting significant anticoagulant and antithrombotic properties. Additionally, P4pal10 reduces carrageenan-induced edema and granulocyte infiltration, and demonstrates protective effects in murine models of myocardial ischemia/reperfusion injury. This compound is valuable for research applications focused on thrombotic disorders and cardiovascular protection.

Parstatin (human) is a potent agonist of the protease-activated receptor 1 (PAR-1), derived from a thrombin receptor peptide. This cell-penetrating compound exhibits significant inhibition of angiogenesis, making it valuable for research into vascular biology and related diseases. Its ability to modulate PAR-1 activity has implications for studies focused on thrombosis, inflammation, and cancer.

ML161 analog 1 is a selective allosteric inhibitor targeting Proteinase-Activated Receptor 1 (PAR1) with an IC50 of 1.68 μM. This compound modulates PAR1 activity, making it a valuable tool for studying its role in various biological processes and disease mechanisms. Its application in research may provide insights into therapeutic strategies involving PAR1.

PAR 4 (1-6) is a hexapeptide that acts as a specific agonist for protease-activated receptor 4 (PAR4). This bioactive compound plays a crucial role in signaling pathways associated with platelet activation and inflammatory responses. Researchers can utilize PAR 4 (1-6) in studies investigating cardiovascular health, hemostasis, and other PAR4-related biological processes.

TRAP-6 amide TFA is a potent agonist of the protease-activated receptor-1 (PAR-1). This peptide activates PAR-1 in response to thrombin, playing a critical role in mediating platelet activation and vascular responses. TRAP-6 amide TFA is commonly used in research applications focused on coagulation, cardiovascular biology, and the study of hemostatic mechanisms.

TRAP-6-IN-1 is a dual inhibitor targeting collagen and TRAP-6, with IC50 values of 17.12 µM and 11.88 µM, respectively. This compound effectively inhibits agonist-induced platelet aggregation in a non-competitive manner, making it a valuable tool for research into platelet function and coagulation disorders. Its dual action may provide insights into therapeutic strategies for cardiovascular diseases associated with platelet hyperactivity.

SLIGRL-NH2 TFA is a potent agonist of Protease-Activated Receptor-2 (PAR-2). It is a peptide that specifically activates PAR-2, facilitating the study of its role in various physiological processes such as inflammation and pain modulation. This reagent is valuable for researchers exploring PAR-2 signaling pathways and their implications in disease mechanisms.

VU0652925 is a potent PAR4 antagonist, demonstrating IC50 values of 43 pM and 39.2 pM for PAC1 and P-selectin, respectively. This compound effectively inhibits GPIIbIIIa activation, making it a valuable tool for investigating the role of PAR4 in platelet activation and related cardiovascular research applications.

PAR-2-IN-2 is a selective inhibitor of protease-activated receptor 2 (PAR-2), exhibiting an IC50 of 10.79 μM against the PAR-2 peptide SLIGKV, while demonstrating a significantly higher IC50 of over 200 μM for Trypsin. This compound is valuable for studying PAR-2 signaling pathways and exploring its role in inflammatory responses and pain modulation. PAR-2-IN-2 serves as a critical tool for researchers investigating therapeutic targets in conditions associated with PAR-2 activation.