Catalog No.
Product Name
Application
Product Information
Citations
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PAR4 antagonist
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. -
PAR-1 Antagonist
Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.- Arundhasa Chandrabalan, .et al. , Am J Physiol Cell Physiol, 2023, Jul 1;325(1):C272-C285 PMID: 37273236
- Arundhasa Chandrabalan, .et al. , Sci Rep, 2023, Jan 20;13(1):1124 PMID: 36670151
- Cansu Tekin, .et al. , Cell Oncol (Dordr), 2020, Aug 18 PMID: 32809114
- Cansu Tekin, .et al. , Oncotarget, 2018, Aug 10; 9(62): 32010-32023 PMID: 30174793
- Claushuis TA, .et al. , J Thromb Haemost, 2017, Apr;15(4):744-757 PMID: 28092405
- Maaike Waasdorp, .et al. , Biochem Biophys Rep, 2017, Jul; 10: 152-156 PMID: 29114573
- Joseph C. Mudd, .et al. , J Infect Dis, 2016, Dec 15; 214(12): 1808-1816 PMID: 27703039
- Corey E. Tabit, .et al. , Circulation, 2016, Jul 12; 134(2): 141-152 PMID: 27354285
- 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.
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PAR4 antagonist
UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM). -
PAR-1 agonist
Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor. -
PAR-1 agonist
iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. iso-TRAP-6 is an analog of TRAP-6 that refers to the use of isoserine instead of serine as first amino acid. -
PAR2 inhibitor
I-287 is an orally active and selective protease-activated receptor 2 (PAR2) inhibitor that functions as a negative allosteric modulator, specifically targeting Gαq and Gα12/13 signaling pathways and their downstream effectors. By disrupting PAR2-mediated signaling, I-287 effectively reduces inflammation in preclinical models, including Complete Freund's Adjuvant (CFA)-induced inflammation in mice. -
PAR2 Antagonist
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. -
PAR-1 Antagonist
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. -
PK2 Antagonist
PKRA83 is a potent antagonist of prokineticin 2 (PK2), functioning by competing for binding sites on PKR1 and PKR2 receptors. It demonstrates significant inhibition of PK2, with IC50 values of 5.0 nM for PKR1 and 8.2 nM for PKR2. PKRA83 exhibits various biological activities, including anticancer, anti-arthritis, and anti-angiogenic effects, making it valuable for research applications in cancer biology, inflammatory diseases, and angiogenesis studies. -
PKR1 Antagonist
PKR1 antagonist 1 is a selective antagonist of the PKR1 receptor, which plays a crucial role in pain signaling. This compound has demonstrated efficacy in reducing hyperalgesia and allodynia in the spared nerve injury (SNI) mouse model. Its application is significant for research focused on pain management and the underlying mechanisms of nociceptive signaling. -
PKR2 Antagonist
A457 is a selective antagonist of the prokineticin receptor PKR2, exhibiting an IC50 value of 102 nM. This compound effectively restores cell surface expression and functionality of the P290S PKR2 variant, while showing no activity against the W178S and G234D PKR2 mutations. A457 is valuable for research applications focused on the modulation of PKR2-related pathways and the study of receptor mutations. -
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.
