Purinergic (P2Y) Receptors

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  1. Cangrelor is a potent intravenous adenosine diphosphate-receptor antagonist
  2. (+)-Clopidogrel hydrogen sulfate is an oral, thienopyridine class antiplatelet agent used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
  3. platelet inhibitor

    Prasugrel is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI.
  4. P2Y14 Receptor Agonist

    MRS2690 is a selective agonist of the P2Y14 receptor, primarily known for its role in the inhibition of adenylyl cyclase activity, which leads to a reduction in intracellular cAMP levels. This compound mediates concentration-dependent vasoconstriction in porcine coronary arteries and induces intracellular calcium mobilization. Additionally, MRS2690 activates p38 MAPK and stimulates [35S]GTPγS binding in RBL-2H3 cell membranes. It also enhances β-hexosaminidase release in response to antigen and complement activation, making it a valuable tool for research in ischemic heart disease.
  5. P2Y1 receptor/[35S]GTPγS binding/β-arrestin 2 recruitment Agonist

    MRS2365 is a highly potent and selective agonist of the P2Y1 receptor, exhibiting an EC50 of 0.4 nM for [35S]GTPγS binding and β-arrestin 2 recruitment. This compound effectively alleviates mechanical allodynia and enhances mechanical sensitivity, making it valuable for pain research. Notably, MRS2365 demonstrates minimal activity at P2Y12 and P2Y13 receptors, highlighting its specificity for P2Y1.
  6. P2Y14R Antagonist

    MK-852 is a potent P2Y14 receptor antagonist that plays a crucial role in modulating platelet aggregation. This compound effectively inhibits the binding of fibrinogen to platelets in vitro, making it a valuable tool for studying thrombotic processes. Research applications include investigations into platelet function and the development of antithrombotic therapies.
  7. P2Y14R Antagonist

    HDL-16 is a highly potent antagonist of the P2Y14 receptor, exhibiting an IC50 of 0.3095 nM. This compound demonstrates significant biological activity by alleviating dextran sulfate sodium (DSS)-induced colitis, primarily through the inhibition of necroptosis in intestinal epithelial cells (IECs) and the preservation of mucosal barrier function. HDL-16 is valuable for research applications focused on inflammatory bowel diseases and related gastrointestinal disorders.
  8. P2Y11 Receptor Agonist

    ATPγS tetralithium salt is a highly effective agonist of the P2Y11 receptor, playing a pivotal role in various cellular signaling pathways. This compound exhibits notable antioxidant properties and provides neuroprotection, enhancing its utility in neuroscience research. Additionally, ATPγS serves as a substrate for nucleotide hydrolysis and RNA unwinding activities mediated by the eukaryotic translation initiation factor eIF4A, making it valuable for studies related to translation and RNA biology. Its activity in ATP hydrolysis further supports its application in metabolic research.
  9. P2Y11 Receptor Agonist

    ATP-γ-S tetrasodium is a potent agonist of the P2Y11 receptor, known for its antioxidant and neuroprotective properties. This compound serves as a substrate for nucleotide hydrolysis and facilitates RNA unwinding activities of the eukaryotic translation initiation factor eIF4A. Additionally, ATP-γ-S tetrasodium demonstrates significant activity in ATP hydrolysis, making it valuable for studies in cellular signaling and translational control.
  10. P2Y14 Agonist

    Uridine 5'-diphosphoglucose disodium is a potent agonist of the P2Y14 receptor, which plays a critical role in the regulation of inflammation and neutrophil polarization in response to ischemic conditions. Secreted by cardiomyocytes, this compound is involved in the synthesis of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in various biological systems. Its ability to modulate inflammatory responses makes Uridine 5'-diphosphoglucose disodium a valuable reagent for studies focused on myocardial infarction and reperfusion-induced inflammation.
  11. P2Y14R Antagonist

    MRS4654 is a potent antagonist of the P2Y14 receptor, with reported inhibitory constants of 15.0 nM for human P2Y14 and 18.6 nM for mouse P2Y14. This compound exhibits significant analgesic and anti-inflammatory properties, making it a valuable tool for investigating pathways involved in pain modulation. MRS4654 is suitable for research applications focused on asthma and neuropathic pain models.
  12. P2Y14 Receptor Agonist

    UDP-Galactose disodium is a potent agonist of the P2Y14 receptor, demonstrating an EC50 of 0.67 μM for the human variant. This compound serves as a substrate for the enzyme beta-1,4 galactosyltransferase V (B4GALT5), playing a critical role in glycosylation processes. Additionally, UDP-Galactose disodium is essential for the biosynthesis of various glycoconjugates that contribute to the surface glycocalyx of Leishmania major, making it valuable for research in cell signaling and pathogen biology.
  13. P2Y2 Receptor Antagonist

    AR-C118925XX is a selective antagonist of the P2Y2 receptor. It effectively inhibits ATP-induced production of interleukin-6 (IL-6) and the phosphorylation of p38 MAPK, key players in inflammatory responses. In vivo studies demonstrate that AR-C118925XX also suppresses Bleomycin-induced dermal fibrosis in mice and inhibits ATP-mediated tumor growth, making it valuable for research in fibrosis, inflammation, and cancer biology.
  14. P2Y12 Receptor Antagonist

    PSB-0739 is a potent, high-affinity competitive antagonist of the P2Y12 receptor, exhibiting a Ki value of 24.9 nM. This receptor is essential for platelet aggregation, and its inhibition may provide valuable insights into antithrombotic therapies. PSB-0739 is suitable for research applications focused on cardiovascular disease and platelet function studies.
  15. P2Y Receptor Agonist

    2-Methylthioadenosine diphosphate trisodium is a potent agonist of purinergic P2Y receptors, specifically exhibiting EC50 values of 19 nM, 6.2 nM, and 5 nM for human P2Y13, mouse P2Y13, and human P2Y12, respectively. Additionally, it demonstrates pEC50 values of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. This compound is known to induce platelet aggregation and morphological changes while inhibiting cyclic AMP accumulation in platelets in the presence of prostaglandin E1, making it a valuable tool for research in platelet function and signaling pathways.
  16. P2Y14-R Antagonist

    PPTN hydrochloride is a selective P2Y14 receptor antagonist characterized by a high-affinity competitive binding with a KB value of 434 pM. This compound exhibits significant anti-inflammatory and anti-immune properties, making it a valuable tool in research related to autoimmune diseases and inflammation pathways. Additionally, PPTN hydrochloride demonstrates no agonist or antagonist effects on other P2Y receptor subtypes, including P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, and P2Y13, ensuring its specificity in biological assays.
  17. P2Y14-R Antagonist

    PPTN is a potent, high-affinity antagonist of the P2Y14 receptor, exhibiting a competitive binding profile with a KB value of 434 pM. This compound demonstrates selectivity by showing no significant agonist or antagonist effects on other P2Y receptors, including P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, and P2Y13. PPTN is useful for research applications focused on anti-inflammatory and immune modulation, providing a valuable tool for studying P2Y14-mediated biological processes.
  18. P2Y11 Antagonist

    NF157 is a selective antagonist of the P2Y11 receptor, exhibiting a pKi of 7.35 and an IC50 of 463 nM. It demonstrates high specificity, with significantly higher IC50 values for related receptors P2Y1 and P2Y2. NF157 is known to reduce the expression of metalloproteinases (MMP)-3 and MMP-13, making it a valuable tool for research into osteoarthritis and related inflammatory conditions.
  19. P2Y12 Receptor Activator

    ADP-β-S trilithium is the trilithium salt form of ADP-β-S, serving as a potent activator of the P2Y12 receptor. It facilitates the upregulation of IL-1β and IL-6 production in microglial cells, promotes NF-κB phosphorylation and nuclear translocation, and enhances NLRP3 inflammasome activation. This reagent is valuable for research into inflammatory responses and signaling pathways involving P2Y12 receptor activation.
  20. P2Y2R/GPR17 Antagonist

    P2Y2R/GPR17 antagonist 1 is a selective antagonist targeting both the P2Y2 receptor (P2Y2R) and G protein-coupled receptor 17 (GPR17), with IC50 values of 3.17 µM and 1.67 µM, respectively. This compound exhibits promising metabolic stability in human liver microsomes, making it a valuable tool for research. It is particularly applicable in studies involving purinergic signaling and neuroinflammation, providing insights into therapeutic strategies for related diseases.
  21. P2Y13 Receptor Antagonist

    MRS 2211 sodium hydrate is a competitive antagonist of the P2Y13 receptor, exhibiting a pIC50 of 5.97. It demonstrates over 20-fold selectivity for the P2Y13 receptor compared to the P2Y1 and P2Y12 receptors. This selective antagonist is valuable for investigating the role of the P2Y13 receptor in various physiological and pathological processes, including its effects in blood cells, the nervous system, and the immune system.
  22. P2Y1 Receptor Antagonist

    MRS2500 tetraammonium is a highly selective antagonist of the P2Y1 receptor, exhibiting a Ki value of 0.78 nM for the recombinant human P2Y1 receptor. This compound effectively inhibits ADP-induced aggregation of human platelets, demonstrating an IC50 of 0.95 nM. MRS2500 tetraammonium is utilized in research applications focused on antithrombotic activity and the modulation of platelet function.
  23. P2Y12 Antagonist

    2-Methylthio-AMP (2-MeSAMP) is a selective antagonist of the P2Y12 receptor, which plays a critical role in mediating platelet aggregation through ADP signaling. This compound effectively inhibits ADP-induced platelet activation, making it a valuable tool for studying platelet function and thrombosis. Its application extends to cardiovascular research, where it can help elucidate the mechanisms underlying platelet aggregation and potential therapeutic strategies for related disorders.
  24. PIT

    P2Y1 Receptor Antagonist

    PIT (2,2'-Pyridylisatogen tosylate) is a selective non-competitive antagonist of the P2Y1 receptor, exhibiting an IC50 value of 0.14 μM for human P2Y1 receptors. It effectively inhibits P2Y1 receptor signaling without interfering with nucleotide binding, demonstrating irreversible antagonism of ATP responses at metabotropic purinoceptors within certain smooth muscle tissues. PIT is valuable for investigating conditions such as chronic bronchitis and asthma, facilitating research into the role of purinergic signaling in these respiratory disorders.
  25. P2Y14R Antagonist

    P2Y14R Antagonist 2 is a potent and selective antagonist of the P2Y14 receptor, demonstrating an IC50 of 0.40 nM. This compound exhibits significant anti-inflammatory properties, making it a valuable tool for research related to colitis and other inflammatory conditions. Its oral bioavailability enhances its applicability in various preclinical studies.
  26. P2Y2 Receptor Agonist

    4-Thiouridine 5′-triphosphate tetralithium is a potent agonist for the P2Y2 and P2Y4 receptors, demonstrating EC50 values of 35 nM and 350 nM, respectively. This UTP analog is utilized in various research applications, including cross-linking experiments and transcriptional complex labeling studies, making it an essential tool for investigating nucleic acid interactions and cell signaling pathways.
  27. P2Y12 Receptor Inhibitor

    (±)-Clopidogrel bisulfate is an inhibitor of the platelet P2Y12 receptor and serves as an adenosine diphosphate (ADP) receptor antagonist. By blocking ADP binding to its receptors on platelet membranes, (±)-Clopidogrel bisulfate effectively attenuates ADP-mediated glycoprotein GPIIb/IIIa complex activation. This compound is utilized in research investigating its role in reducing vascular inflammation and mitigating the progression of angiotensin II-induced abdominal aortic aneurysms, as well as exploring its anti-inflammatory properties.
  28. P2Y Receptor Inhibitor

    PSB-16133 sodium is a potent P2Y receptor inhibitor that selectively targets various P2Y receptor subtypes. This compound is valuable for studying purinergic signaling pathways and understanding their roles in physiological and pathological processes. PSB-16133 sodium can be utilized in research applications focusing on inflammation, cardiovascular disorders, and neuronal signaling.
  29. P2Y Receptor Antagonist

    Selatogrel is a reversible and selective P2Y12 receptor antagonist, effectively inhibiting platelet aggregation with an IC50 of 8 nM. This compound demonstrates significant antithrombotic activity, making it a valuable tool for research in cardiovascular disease, particularly in studies focused on thrombus formation and prevention. Selatogrel's specific mechanism of action allows for targeted investigations into the role of platelet inhibition in various pathological conditions.
  30. P2Y1/P2Y12 Antagonist

    P2Y1/P2Y12 antagonist-1 is a dual inhibitor targeting the P2Y1 and P2Y12 receptors, providing significant antiplatelet activity. This compound effectively inhibits ADP-induced platelet aggregation in rabbit plasma, demonstrating an IC50 value of 4.23 μM. Additionally, P2Y1/P2Y12 antagonist-1 shows potent inhibitory effects in a rat thrombosis model, making it a valuable tool for research on platelet function and related cardiovascular conditions.
  31. P2Y₁₂ Receptor Inhibitor

    R-138727 is a potent and selective irreversible antagonist of the P2Y12 receptor, functioning as a key inhibitor with an IC50 of 2.5 μM. This compound covalently binds to the P2Y12 receptor present on platelet surfaces, effectively blocking adenosine diphosphate-mediated platelet activation and aggregation. R-138727 is valuable for research applications targeting stroke, cerebral infarction, and associated neurological deficits.
  32. P2Y1 Receptor Antagonist

    MRS2279 diammonium is a selective antagonist of the P2Y1 receptor, exhibiting high affinity with a Ki value of 2.5 nM and an IC50 of 51.6 nM. This compound competitively inhibits ADP-induced platelet aggregation, demonstrated by a pKb value of 8.05. MRS2279 diammonium is valuable for studies investigating platelet function and thrombotic diseases.
  33. P2Y1 Receptor Antagonist

    MRS2179 tetrasodium is a competitive antagonist of the P2Y1 receptor, demonstrating a Kb value of 102 nM and a pA2 of 6.99 for the turkey P2Y1 receptor. This compound exhibits selectivity for P2Y1 over other purinergic receptors, including P2X1 (IC50 = 1.15 µM) and P2X3 (IC50 = 12.9 µM). MRS2179 tetrasodium is particularly useful in studies of platelet aggregation and various signaling pathways involving purinergic receptors.
  34. P2Y2R Agonist

    MRS2768 tetrasodium salt is a selective agonist for the P2Y2 receptor. This compound demonstrates protective effects on cardiomyocytes against ischemic damage both in vivo and in vitro, making it a valuable tool for research into cardiovascular diseases. Its ability to activate P2Y2 receptors can aid in studying various biological processes related to cell survival and tissue protection.
  35. P2Y12 Receptor Antagonist

    Regrelor disodium is a reversible antagonist of the P2Y12 receptor, functioning as a competitive inhibitor of ADP. This compound demonstrates significant inhibitory effects on platelet activation and aggregation, making it valuable in studies focusing on thrombus formation and cardiovascular disease. Additionally, Regrelor disodium has been shown to inhibit cell proliferation, thereby finding applications in inflammation-related research.
  36. P2Y12 Antagonist

    2-Methylthio-AMP diTEA is a selective and direct antagonist of the P2Y12 receptor. This compound effectively inhibits ADP-dependent platelet aggregation, making it a valuable tool for studying platelet function and thrombosis-related pathways in cardiovascular research. Its specificity for the P2Y12 receptor allows for detailed exploration of purinergic signaling and potential therapeutic applications in platelet-mediated disorders.
  37. P2Y1 Antagonist

    Adenosine 2',5'-diphosphate sodium is a competitive antagonist of the P2Y1 receptor. It demonstrates non-selective antagonistic activity at both recombinant and human platelet P2X1 receptors. This compound is useful in research applications focusing on purinergic signaling pathways and the modulation of platelet activation.
  38. P2Y11 Agonist

    NF546 is a selective non-nucleotide agonist of the P2Y11 receptor, exhibiting a pEC50 of 6.27. This compound effectively stimulates the release of interleukin-8 from human monocyte-derived dendritic cells, making it valuable for research focused on immune response modulation and inflammation pathways. Its targeted action on P2Y11 highlights its potential in studying purinergic signaling and associated biological functions.
  39. P2X1/ P2Y1 Receptor Antagonist

    Blue FPG-A trisodium is a selective antagonist of the P2X1 and P2Y1 receptors, exhibiting IC50 values of 35.5 μM and 2.6 μM, respectively. This compound serves as a valuable tool for investigating purinergic signaling pathways and their implications in various physiological and pathological processes. Its structural relationship to Reactive Blue 2 (RB2) further supports its utility in biochemical assays and research applications focused on receptor interactions and cellular signaling mechanisms.
  40. P2Y2/P2Y4 Agonist

    Uridine-5'-O-(3-thiotriphosphate) trisodium is a stable analogue of UTP that acts as a potent agonist of the P2Y2 and P2Y4 receptors. Its increased metabolic stability enhances its effectiveness in various biological studies. This compound is valuable for research applications involving purinergic signaling and receptor physiology.
  41. P2Y12 Receptor Antagonist

    SAR216471 hydrochloride is a potent P2Y12 receptor antagonist that exhibits significant antiplatelet and antithrombotic activities in vivo. By inhibiting P2Y12 receptor signaling, it offers valuable insights into the mechanisms of platelet activation and thrombosis. This compound is suitable for research applications studying cardiovascular diseases and thromboembolic disorders.
  42. P2Y1 Antagonist

    BMS-884775 is a potent and selective antagonist of the P2Y1 receptor, exhibiting an IC50 of 0.1 nM for the human target. This compound demonstrates significant antiplatelet activity, effectively preventing arterial thrombosis while minimizing bleeding risk and duration compared to other antiplatelet agents. BMS-884775 is a valuable tool for research in the fields of cardiovascular disease and arterial thrombosis management, offering insights into therapeutic strategies for related health conditions.
  43. P2Y12 Receptor Ligand

    PSB-22219 is a highly selective non-nucleotidic ligand for the P2Y12 receptor, with a binding affinity of KD=4.57 nM. This compound demonstrates significant promise in the study of P2Y12 receptor-mediated neuroinflammation, making it a valuable tool for research applications in neurobiology and related fields. Its specificity and efficacy facilitate investigations into the role of P2Y12 in various pathological conditions.
  44. P2Y6R Agonist

    UTPU trisodium is a selective agonist of the P2Y6 receptor, exhibiting an EC50 of 0.4 μM. This compound effectively activates intracellular calcium signaling pathways mediated by P2Y6, making it a valuable tool for studying inflammatory processes. UTPU trisodium is suitable for research applications focused on inflammation and related signaling mechanisms.
  45. P2Y1 Receptor Antagonist

    MRS-2179 is a selective competitive antagonist of the P2Y1 receptor, exhibiting a binding affinity with a KB value of 0.177 μM. This compound plays a crucial role in molecular research focused on purinergic signaling, enabling the investigation of cellular responses mediated by ATP. MRS-2179 is valuable for studying its implications in various physiological and pathological processes, including cardiovascular function and platelet aggregation.
  46. P2Y Receptor Agonist

    MRS2957 is a selective agonist of the P2Y6 receptor, which plays a crucial role in activating AMP-activated protein kinase (AMPK) in pancreatic β-cells. This activation promotes insulin secretion while reducing apoptosis, highlighting its potential as a therapeutic target for type 2 diabetes. MRS2957 may provide valuable insights in research focused on diabetes treatment and pancreatic function.
  47. P2Y₁₄ Receptor Agonist

    UDP-Galactose is a glycosyl donor molecule and a natural agonist of the P2Y14 receptor, which is coupled to Gi proteins in immune responses. It exhibits significant biological activity with an IC50 value of 0.67 μM for human P2Y14 receptor activation. This reagent is valuable for research applications investigating cell signaling pathways and nucleotide sugar metabolism.
  48. P2Y12 Receptor Antagonist

    AR-C66096 is a selective antagonist of the Gi-coupled P2Y12 receptor, known for its potent ability to inhibit ADP-induced platelet aggregation. This compound effectively reduces thrombus stability under physiological flow conditions, making it a valuable tool for antithrombotic research. Its application in studying platelet function and thrombus formation can provide insights into cardiovascular diseases and therapeutic interventions.
  49. P2Y11 Receptor Inhibitor

    NF340 is a selective inhibitor of the P2Y11 receptor, achieving a pIC50 of 7.3-7.7 in human cells. It effectively blocks nociceptive signaling and alleviates the upregulation of P2Y11 receptors in the spinal dorsal horn following spinal cord injury. NF340 further inhibits the NFκB signaling pathway induced by IL-1β, leading to a reduction in pro-inflammatory cytokine expression and a decrease in intracellular ROS levels. Additionally, it suppresses ATP-induced calcium influx and cell migration in human hepatocellular carcinoma cells. NF340 is relevant for research into neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis, and hepatocellular carcinoma.
  50. P2Y4 Receptor Agonist

    mrs 4062 TEA is a selective agonist of the P2Y4 receptor, exhibiting a potent EC50 of 23 nM. This compound also demonstrates moderate activity against the P2Y2 and P2Y6 receptors, with EC50 values of 640 nM and 740 nM, respectively. mrs 4062 TEA is valuable in research focused on purinergic signaling and its implications in various physiological processes and disease states.

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