Protease-Activated Receptors (PAR)

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.

AC-264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5).

BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively.

ML-161 is an 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).

AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation.

AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.

I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.

GB110 is a Novel potent non-peptide PAR2 agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.

GB-88 is a novel selective, orally available PAR2 antagonist, inhibits PAR2 activated Ca2+ release with an IC50 of 2 ?M.

UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM).

Thrombin Receptor Activator for Peptide 5 (TRAP-5), coagulation factor II (thrombin) receptor is a G protein-coupled receptor involved in the regulation of thrombotic response.

ENMD-1068 hydrochloride is a selective antagonist of protease-activated receptor 2 (PAR2). This compound effectively reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling pathways. Additionally, ENMD-1068 hydrochloride demonstrates the ability to inhibit the proliferation of endometrial cells and induce apoptosis in epithelial cells associated with lesions. This reagent is valuable for research applications in endometriosis and liver fibrosis.

Atopaxar is a selective and reversible antagonist of the thrombin receptor protease-activated receptor-1 (PAR-1). By inhibiting PAR-1 signaling, Atopaxar serves as an effective antiplatelet agent, disrupting platelet activation and aggregation. This compound is valuable for research applications related to atherothrombotic diseases, providing insights into the mechanisms of platelet-mediated thrombosis and potential therapeutic interventions.

Atopaxar hydrochloride is a selective and reversible antagonist of protease-activated receptor-1 (PAR-1) that functions primarily as a thrombin receptor inhibitor. This compound demonstrates significant biological activity by inhibiting Janus kinase 1 (JAK1) and JAK2, resulting in JAK-STAT pathway inhibition with an EC50 of 5.90 μM in A549 cells. It has been shown to decrease cell viability (IC50=7.02 μM), induce apoptosis, and arrest the cell cycle at the G1 phase. Atopaxar hydrochloride is valuable in research focused on atherothrombotic diseases and exhibits both antiplatelet and antitumor properties.