Catalog No.
Product Name
Application
Product Information
Citations
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PAR-1 Antagonist
SCH-602539 is a selective antagonist of the protease-activated receptor 1 (PAR-1). It effectively inhibits platelet aggregation induced by PAR-1-selective thrombin receptor agonists, making it a valuable tool in studying thrombotic mechanisms. SCH-602539 has demonstrated synergistic antithrombotic effects when used in conjunction with other agents such as Cangrelor, highlighting its potential applications in cardiovascular research and drug development. -
PAR2 Antagonist
AZ8838 is a potent, competitive allosteric antagonist of proteinase-activated receptor 2 (PAR2), exhibiting a pKi of 6.4 for human PAR2. This non-peptide small molecule displays significant inhibitory activity, making it valuable for research investigating PAR2-related pathophysiological processes. Its oral bioavailability enhances its utility in in vivo studies focused on pain, inflammation, and other PAR2-mediated conditions. -
PAR1 Antagonist
PZ-128 is a specific and reversible antagonist of protease-activated receptor-1 (PAR1), functioning as a cell-penetrating lipopeptide pepducin. By targeting the cytoplasmic surface of PAR1, PZ-128 effectively interrupts signaling to internally-located G proteins. This compound exhibits significant biological activities, including antiplatelet, anti-metastatic, anti-angiogenic, and anticancer effects, making it beneficial for research applications in cardiovascular and cancer biology. -
PAR1 Agonist
TFLLR-NH2 (TFA) is a selective agonist of the Protease-Activated Receptor-1 (PAR1), exhibiting an EC50 of 1.9 μM. It effectively activates PAR1-mediated signaling pathways, making it a valuable tool for investigating thrombin-related physiological processes. This compound is suitable for research applications in vascular biology, platelet function studies, and the exploration of cardiovascular disease mechanisms. -
PAR4 Antagonist
BMS-986141 is a selective antagonist of the protease-activated receptor-4 (PAR-4) that exhibits an IC50 value of 0.4 nM. This compound demonstrates strong antithrombotic properties, making it a valuable tool for research within the fields of cardiovascular disease and thrombus formation. Its oral bioavailability enhances its utility in preclinical studies aimed at understanding the role of PAR-4 in various physiological and pathological processes. -
PAR-1 Antagonist
Vorapaxar sulfate is a selective antagonist of protease-activated receptor-1 (PAR-1), demonstrating competitive inhibition with a Ki value of 8.1 nM. This antiplatelet agent effectively inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner. Vorapaxar sulfate is utilized in research focused on thrombotic disorders and cardiovascular diseases, providing insights into platelet activation and aggregation pathways. -
PAR2 Inhibitor
PAR-2-IN-1 is a selective inhibitor of protease-activated receptor-2 (PAR2), targeting the PAR2 signaling pathway. This compound exhibits significant anti-inflammatory and anticancer properties, making it a valuable tool in research. Its capabilities provide insights into the role of PAR2 in various biological processes and diseases, facilitating the investigation of therapeutic interventions in inflammation and cancer. -
PAR2 Antagonist
GB83 is a potent antagonist of protease-activated receptor 2 (PAR2). It effectively reverses neutrophil elastase-induced synovitis and alleviates associated pain. Additionally, GB83 inhibits the impact of MET-1 supernatant on NG neurons, making it a valuable tool for research into inflammatory responses and neurobiology. -
PAR1 Agonist
TFLLR-NH2 is a selective agonist of the protease-activated receptor 1 (PAR1), exhibiting an EC50 value of 1.9 μM. This compound activates PAR1, a key receptor involved in various physiological processes, including inflammation and thrombosis. TFLLR-NH2 is valuable for research applications focused on the role of PAR1 in cellular signaling pathways and its implications in cardiovascular and neurological conditions. -
PAR4 Antagonist
tcY-NH2 TFA is a potent selective antagonist of the protease-activated receptor 4 (PAR4). This peptide effectively inhibits thrombin- and AY-NH2-induced platelet aggregation as well as endostatin release. tcY-NH2 TFA is valuable for research in the fields of inflammation and immunology, providing insights into platelet function and related signaling pathways. -
PAR4 Antagonist
tcY-NH2 is a selective antagonist of the protease-activated receptor 4 (PAR4), functioning through modulation of thrombin action. This peptide effectively inhibits both thrombin- and AY-NH2-mediated platelet aggregation as well as endostatin release. tcY-NH2 is valuable for investigations related to inflammation and immunology, providing insights into the role of PAR4 in various physiological and pathological processes. -
PAR Agonist
Protease-Activated Receptor-4 is an agonist for proteinase-activated receptor-4 (PAR4). It plays a crucial role in mediating platelet activation and inflammatory responses. This compound is valuable for research in cardiovascular diseases and the study of thrombo-inflammatory processes. -
PAR Antagonist
ML354 is a selective antagonist of the protease-activated receptor 4 (PAR4), exhibiting an IC50 of 140 nM. This compound effectively inhibits PAR4 signaling, making it valuable for research into coagulation, inflammation, and thrombosis. ML354's specificity for PAR4 offers potential applications in studying the receptor's role in various physiological and pathological processes. -
PAR Agonist
VKGILS-NH2 is a reversed amino acid sequence designed as a control peptide for SLIGKV-NH2, a known protease-activated receptor 2 (PAR2) agonist. This compound serves as a valuable tool in studies investigating PAR2 signaling pathways, while demonstrating no impact on DNA synthesis in cellular assays. Its application facilitates the exploration of receptor-specific functions and contributes to a deeper understanding of PAR2-related biological processes. -
Platelets Activator
PAR-4 (1-6) amide (human) is an N-terminal peptide fragment of protease-activated receptor 4 (PAR4) that acts as a platelet activator. This compound induces platelet aggregation, making it valuable for research involving hemostasis and thrombosis. It serves as a useful tool in studies aimed at understanding platelet function and the signaling pathways associated with cardiovascular diseases. -
TRAP/ACP5 Inhibitor
CBK289001 is an inhibitor of tartrate-resistant acid phosphatase (TRAP/ACP5). It effectively inhibits TRAP 5bMV, TRAP 5bOX, and TRAP 5aOX with IC50 values of 125 µM, 4.21 µM, and 14.2 µM, respectively. This compound is useful for studying the role of TRAP in various biological processes and may aid in the development of therapeutic strategies targeting TRAP-related pathways. -
Mast Cell Tryptase Inhibitor
APC 366 TFA is an irreversible inhibitor of mast cell tryptase, a key enzyme involved in allergic responses. This reagent is instrumental in research focused on allergic diseases and related inflammatory processes. Its ability to effectively inhibit tryptase makes it a valuable tool for studying the mechanisms underlying mast cell activation and associated pathologies. -
PAR1 Antagonist
FR-171113 is a specific non-peptide antagonist of the protease-activated receptor 1 (PAR1). This compound demonstrates significant antithrombotic effects by inhibiting thrombin-induced platelet aggregation, with an IC50 value of 0.29 µM. FR-171113 is valuable for research applications focused on cardiovascular diseases and platelet function studies. -
PAR4 Antagonist
PAR4 Antagonist 5 is a selective inhibitor of the protease-activated receptor 4 (PAR4) that exhibits an IC50 of less than 20 μM. This compound demonstrates significant anti-platelet aggregation activity, making it a valuable tool for investigating thrombotic diseases. Its utility in research applications related to cardiovascular conditions and hemostasis offers insights into the modulation of platelet function. -
PAR 1 Agonist
TRAP-5 amide is a protease-activated receptor 1 (PAR 1) agonist peptide. This compound is utilized extensively in research focusing on platelet activation and thrombotic processes due to its ability to trigger PAR 1 signaling pathways. TRAP-5 amide serves as a vital tool for investigating cardiovascular diseases and studying the molecular mechanisms underlying hemostasis and inflammation. -
PAR4 Inhibitor
PAR4 Antagonist 4 is a selective inhibitor of protease-activated receptor 4 (PAR4), demonstrating potent antiplatelet activity with an IC50 of 14.2 nM. This compound exhibits enhanced metabolic stability in human liver microsomes, with a half-life (T1/2) of 42.5 minutes. PAR4 Antagonist 4 is suitable for research applications focused on hemostasis, cardiovascular disorders, and the modulation of platelet activation pathways. -
Protease-Activated Receptor 4 Antagonist
PAR4 Antagonist 1 is a potent antagonist of Protease-Activated Receptor 4 (PAR4), exhibiting an IC50 of 1.8 nM. It effectively inhibits γ-thrombin-activated PAR4 in platelet-rich plasma with an IC50 of 2 nM. This compound is suitable for research applications focused on antithrombotic mechanisms and the modulation of platelet activation pathways. -
PAR-1 Agonist
Parstatin (mouse) is a cell-penetrating peptide that acts as an agonist for the protease-activated receptor 1 (PAR-1). This compound has been shown to effectively inhibit angiogenesis, making it a valuable tool in the study of vascular biology and related diseases. Its ability to modulate PAR-1 activity positions it for research applications in cancer, wound healing, and other angiogenesis-related conditions. -
Protease Activated Receptor (PAR)
PAR3 (1-6) is a synthetic peptide that functions as an agonist for the protease-activated receptor (PAR1). This peptide corresponds to the first six residues of the amino-terminal tethered ligand sequence from human PAR3 and residues 39-44 from the full-length human sequence. PAR3 (1-6) effectively activates p42/44 MAPK signaling pathways in fibroblasts that express PAR1, an activation that can be inhibited by the PAR1 antagonist RWJ 56110. This reagent is valuable for research involving receptor signaling mechanisms and cellular responses to proteolytic activation. -
PAR-1 Agonist
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a selective agonist for Protease-Activated Receptor 1 (PAR-1), distinguishing it from PAR-2. This bioactive peptide mediates the cellular effects associated with thrombin and plays a significant role in various thrombin-related cellular activities. Furthermore, PAR-1 is implicated in the regulation of thrombin-induced hepatocellular carcinoma, highlighting its relevance in tumor microenvironments characterized by coagulation factors. This compound is essential for studies focusing on PAR-1 signaling pathways and thrombin-related pathophysiology. -
PAR-2 Antagonist
PAR-2 antagonist 1 is a selective antagonist of protease-activated receptor 2 (PAR2), exhibiting an inhibitory concentration IC50 value of 0.9 μM. This compound effectively blocks PAR2 signaling, which is implicated in the proliferation and migration of breast cancer cells. PAR-2 antagonist 1 is valuable for research applications focused on understanding PAR2's role in cancer biology and exploring potential therapeutic strategies for breast cancer treatment. -
PAR4 Inhibitor
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. -
PAR1 Antagonist
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. -
PAR-1 Antagonist
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. -
PAR Agonist
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. -
PAR Agonist
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. -
PAR2 Antagonist
(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. -
Protease Activated Receptor (PAR) Antagonist
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. -
PAR2 Antagonist
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. -
PAR4 Antagonist
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. -
PAR-1 Agonist
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. -
PAR1 Allosteric Inhibitor
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. -
PAR4 Agonist
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. -
PAR-1 Agonist
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. -
Collagen/TRAP-6 Inhibitor
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. -
PAR Agonist
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. -
PAR4 Antagonist
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 Inhibitor
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. -
NPY Y1/NPFF Receptor Antagonist
BIBP3226 is a selective antagonist of the neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptors, exhibiting K_i values of 1.1 nM, 79 nM, and 108 nM for rat NPY Y1, human NPFF2, and rat NPFF, respectively. This compound has demonstrated anxiogenic-like effects, making it a valuable tool for research in neuropharmacology, particularly in studies exploring anxiety-related disorders and the modulation of neuropeptide signaling pathways. -
NPY Y5 antagonist
S 25585 is a selective antagonist of the neuropeptide Y (NPY) Y5 receptor. This compound is primarily utilized in research focused on appetite regulation, demonstrating a significant ability to reduce food intake without directly blocking the Y5 receptor. Its unique mechanism makes it an essential tool for studying the intricate pathways involved in energy homeostasis and metabolic disorders. -
NPY-5 Receptor Antagonist
Neuropeptide Y5 receptor ligand-1 is a potent antagonist of the neuropeptide Y5 (NPY-5) receptor. This carbazole derivative is utilized in research applications focused on the role of NPY-5 in various physiological processes, including regulation of appetite, anxiety, and circadian rhythms. By inhibiting NPY-5 receptor activity, it provides valuable insights into neuropeptide signaling pathways and their implications in metabolic and neurobehavioral disorders. -
NPY-5 Receptor Antagonist
NPY-5 receptor antagonist-1 is a potent antagonist of the neuropeptide Y5 (NPY-5) receptor, exhibiting a Ki value of less than 1 μM. This compound is invaluable for investigating the roles of NPY-5 in obesity, feeding disorders, and various neurological conditions. Its ability to modulate NPY-5 receptor activity makes it a useful tool in pharmacological research and drug development related to metabolic and neuropsychiatric disorders. -
NPY Y5 Receptor Agonist
(D-Trp32)-Neuropeptide Y (porcine) is a selective agonist of the neuropeptide Y (NPY) Y5 receptor. It exhibits orexigenic activity, thereby promoting increased food intake, and has been shown to inhibit Forskolin-stimulated cAMP formation. This peptide is valuable for research focusing on appetite regulation and metabolic disorders. -
NPY Y1 Receptor Antagonist
BVD 10 is a highly selective antagonist of the neuropeptide Y (NPY) Y1 receptor. This compound effectively inhibits NPY-induced increases in glutamate levels, providing insights into neurochemical interactions. BVD 10 is particularly valuable for research focused on seizure mechanisms and related neurological studies. -
NPY Receptor Antagonist
BIIE-0246 dihydrochloride is a potent and highly selective non-peptide antagonist of the neuropeptide Y (NPY) Y2 receptor, exhibiting an IC50 value of 15 nM. This compound effectively inhibits NPY signaling, making it valuable for research on appetite regulation, neuroprotection, and anxiety-related disorders. BIIE-0246 dihydrochloride provides a robust tool for investigating the physiological roles of NPY and its involvement in various pathophysiological conditions.
