Purinergic (P2Y) Receptors

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  1. P2Y14R Antagonist

    MRS4833 is a potent, orally active antagonist of the P2Y14 receptor, exhibiting competitive inhibition with IC50 values of 5.92 nM for human and 4.8 nM for mouse P2Y14R. This compound effectively reduces airway eosinophilia in protease-mediated asthma models and has demonstrated the ability to reverse chronic neuropathic pain in mouse models of chronic constriction injury. MRS4833 is valuable for research investigating P2Y14R-related pathways in asthma and pain management.
  2. P2Y12 Antagonist

    2-Methylthio-AMP sodium is a selective antagonist of the P2Y12 receptor, known for its inhibitory effects on ADP-dependent platelet aggregation. This compound is utilized in research focused on thrombus formation and cardiovascular diseases, providing insights into platelet function and potential therapeutic interventions for thrombotic disorders. Its specificity for P2Y12 makes it a valuable tool in understanding the mechanisms of platelet activation and inhibition.
  3. P2Y1 Antagonist

    P2Y1 Antagonist 4 is a selective antagonist of the P2Y1 receptor, demonstrating significant inhibition of receptor-mediated cytosolic calcium increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets. This compound effectively penetrates the blood-brain barrier and has been shown to upregulate nuclear Nrf2 protein levels in H2O2-treated HT22 cells. Additionally, P2Y1 Antagonist 4 reduces myocardial infarct size in a mouse model of acute myocardial infarction, making it a valuable tool for research in ischemic stroke and myocardial infarction.
  4. P2Y receptor Agonist

    2-MeSADP is a potent agonist for P2Y receptors, exhibiting an EC50 of 5 nM for human P2Y12 and EC50 values of 19 nM and 13 nM for human P2Y13, with an EC50 of 6.2 nM for mouse P2Y13. This compound preferentially activates P2Y12 over P2Y13 and induces increases in intracellular calcium levels, Gi-mediated cAMP inhibition, and adenylate cyclase inhibition, facilitating downstream signaling pathways. 2-MeSADP is suitable for investigations into various biological processes, including research related to glaucoma.
  5. P2Y14 Receptor Antagonist

    MRS4608 is a selective antagonist of the P2Y14 receptor, exhibiting IC50 values of 20 nM for the human P2Y14 receptor and 21.4 nM for the mouse counterpart. This compound demonstrates anti-inflammatory properties and has been shown to reduce eosinophil infiltration. MRS4608 is valuable for research in inflammation and immunology, with specific applications in studies related to asthma.
  6. P2Y Receptor Agonist

    2-Thio-UTP tetrasodium is a potent agonist of the P2Y2, P2Y4, and P2Y6 receptors. It plays a crucial role in cell signaling pathways involved in cancer research, facilitating the study of tumor microenvironments and cellular responses. This compound is valuable for investigating therapeutic targets related to purinergic signaling in various cancers.
  7. P2Y12 Antagonist

    SAR216471 is a selective P2Y12 receptor antagonist that reversibly inhibits the binding of 2MeSADP to P2Y12 receptors, demonstrating an IC50 of 17 nM in vitro. This compound effectively inhibits platelet aggregation and displays anti-thrombotic activity in rat models. SAR216471 is pertinent for investigations into thrombosis and related cardiovascular research applications.
  8. P2Y Receptor Antagonist

    MRS4865 is a selective antagonist of the P2Y14 receptor, designed to inhibit its biological activity. This compound demonstrates significant potential in mitigating neuropathic pain through its unique dual mechanism, which combines antagonist properties with UDP-glucose agonist functionality. MRS4865 is suitable for research applications exploring pain pathways and P2Y receptor signaling, making it a valuable tool for studying neuropharmacology and therapeutic interventions for pain management.
  9. P2Y14-R Antagonist

    PPTN mesylate is a selective antagonist of the P2Y14 receptor, demonstrating a high affinity with a KB value of 434 pM. It exhibits no agonistic or antagonistic effects on other P2Y receptor subtypes, including P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13. This compound has potential applications in research focused on anti-inflammatory and immune modulation mechanisms.
  10. P2Y12 Receptor Antagonist

    Becondogrel is a P2Y12 receptor antagonist that functions as a potent metabolite of Clopidogrel. It irreversibly inhibits the P2Y12 receptor, leading to the inhibition of platelet aggregation and thrombosis. This compound is valuable for research in cardiovascular diseases and thrombotic disorders, providing insights into antiplatelet therapies and the mechanisms underlying platelet function.
  11. P2Y Receptor Antagonist

    MRS2567 is a selective antagonist of P2Y receptors, effectively inhibiting the contraction of mouse mesenteric arteries. This compound disrupts sustained contractions induced by UTP and UDP, and modulates the Na+, K+, 2Cl- co-transport-dependent signaling pathway, thereby influencing the myogenic tone in these blood vessels. MRS2567 is valuable for research into vascular function and receptor signaling mechanisms.
  12. P2Y1 Receptor Antagonist

    MRS2279 is a selective antagonist of the P2Y1 receptor, demonstrated by a Ki value of 2.5 nM and an IC50 of 51.6 nM. This compound effectively inhibits ADP-induced platelet aggregation in a competitive manner, with an apparent affinity of pKB = 8.05. MRS2279 is valuable for research applications involving platelet function and signaling pathways related to purinergic receptors.
  13. P2YR Activator

    Sp-UTP-α-S (Uridine 5'-O-1-thiotri-phosphate) functions as an activator of P2Y2 and P2Y4 receptors. This compound is particularly useful in cancer research, where it can help elucidate the roles of purinergic signaling in tumor biology. By activating these receptors, Sp-UTP-α-S may contribute to studies related to cell proliferation, migration, and signaling pathways associated with cancer progression.
  14. P2Y2 Receptor Agonist

    PSB-1114 tetrasodium is a potent agonist of the P2Y2 receptor, exhibiting an EC50 of 134 nM and demonstrating significant enzymatic stability. This compound is highly selective, showing over 50-fold selectivity against the P2Y4 and P2Y6 receptors, with EC50 values of 9.3 μM and 7.0 μM, respectively. PSB-1114 tetrasodium is valuable for research applications focusing on P2Y2 receptor-mediated signaling pathways and related physiological processes.
  15. P2Y12 Receptor Antagonist

    MRS2395 is a potent antagonist of the P2Y12 receptor, a key regulator of platelet activity. It effectively inhibits ADP-induced platelet activation with a half-maximal inhibitory concentration (Ki) of 3.6 μM and suppresses cAMP production in rat platelets in the presence of PGE1 with an IC50 of 7 µM. Additionally, MRS2395 promotes the release of dense granules from platelets in response to TRAP-6, making it a valuable tool for research into platelet function and thrombotic disorders.
  16. P2Y6 Receptor Agonist

    5-OMe-UDP, a potent P2Y6 receptor agonist with an EC50 of 0.08 μM, activates the P2Y6 receptor by binding and initiating intracellular signaling cascades. This activation results in increased intracellular calcium ion concentration, influencing various cellular functions. The presence of methoxy groups in 5-OMe-UDP enhances its selectivity and activity, making it a valuable tool for investigating pathologies associated with P2Y6 receptor function, including diabetes, inflammatory bowel disease, and Alzheimer's disease.
  17. P2Y2/P2Y4 Agonist

    Uridine-5'-O-(3-thiotriphosphate) (UTPγS) is a stable analogue of Uridine triphosphate (UTP) that acts as a potent agonist for the P2Y2 and P2Y4 receptors. It demonstrates significant biological activity by stimulating inositol phosphate formation in human 1321N1 astrocytoma cells that express the phospholipase C-coupled human P2U-purinoceptor, with an EC50 value of 240 nM. This compound is valuable for research applications focused on purinergic signaling and receptor pharmacology.
  18. P2Y1R Antagonist

    Desmodilactone is an allosteric antagonist of the P2Y1 receptor. It exhibits significant potential in modulating platelet activation and aggregation, thereby contributing to research on thrombosis and related cardiovascular conditions. This compound can be utilized in studies aimed at understanding P2Y1 signaling pathways and developing targeted therapies for thrombotic diseases.
  19. P2Y12 Antagonist

    ACT-281959 is an orally bioavailable prodrug of Selatogrel, functioning as a P2Y12 receptor antagonist. This reagent effectively inhibits platelet aggregation, making it a valuable tool for investigating cardiovascular diseases and related pathophysiological mechanisms. Its utility in research can aid in the development of therapeutic strategies targeting thrombotic disorders.
  20. P2Y1 Antagonist

    P2Y1 antagonist 1 is a highly effective antagonist of the P2Y1 receptor, exhibiting IC50 values of 1.1 nM in the FLIPR assay and 0.24 μM in the hPA assay. This compound is crucial for advancing antiplatelet research, providing insights into the modulation of platelet activation and implications for cardiovascular therapeutics. Its potent inhibitory action makes it a valuable tool for studying P2Y1-related biological pathways.
  21. P2Y1 Antagonist

    Adenosine 3'-phosphate 5'-phosphosulfate is a selective antagonist of the P2Y1 receptor, effectively inhibiting ADP-induced platelet aggregation without affecting P2Y2, P2Y4, or P2Y6 receptors. This compound disrupts the ability of ADP to induce shape change and elevate intracellular Ca2+ levels in platelets while not influencing ADP's inhibition of adenylate cyclase. In addition to its antagonistic properties, Adenosine 3'-phosphate 5'-phosphosulfate serves as a co-substrate for glycan sulfonation, and can be utilized in Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays for sulfonate group transfer.
  22. P2Y2/P2Y4 Activator

    Ap4C tetrasodium is an activator of P2Y2 and P2Y4 receptors, functioning as a signaling molecule through its interaction with these purinergic receptors. It induces platelet aggregation and mediates various cellular responses, making it a key reagent in the study of inflammation and blood coagulation pathways. This compound is valuable for research applications focusing on the pharmacology of platelet function and related vascular processes.
  23. P2Y Receptor Antagonist

    P2Y12 antagonist 1 is a P2Y12 receptor antagonist, exhibiting a Ki of 3.13 μM. This compound effectively inhibits platelet aggregation, making it a promising candidate for antithrombotic applications in cardiovascular research. Its role in modulating P2Y12 receptor activity highlights its potential for investigating platelet function and thrombus formation.
  24. P2Y1/13 Receptor Antagonist

    MRS2603 is a pyridoxal derivative that acts as a potent antagonist of the P2Y1 and P2Y13 receptors. This compound exhibits significant biological activity by inhibiting the signaling pathways mediated by these purinergic receptors. MRS2603 is valuable for research applications involving the modulation of purinergic signaling and the study of various physiological processes and disease mechanisms associated with P2Y receptor activity.
  25. P2Y1 Receptor Antagonist

    MRS2496 is a selective antagonist of the P2Y1 receptor, exhibiting an IC50 value of 1.5 μM. This compound effectively demonstrates antiplatelet aggregation activity, making it a valuable tool in the study of antiplatelet mechanisms. MRS2496 is applicable in research focused on blood-related diseases, offering insights into therapeutic strategies for conditions involving platelet function.
  26. P2Y14 Receptor Agonist

    UDP-GlcNAc serves as a full agonist of the P2Y14 receptor, a key mediator in various cellular signaling pathways. It plays a crucial role in inhibiting adenosine 3',5'-monophosphate (cAMP) formation, providing insight into metabolic processes and receptor signaling. This compound is particularly valuable in research related to bacterial infections and the study of peptidoglycan biosynthesis.
  27. Purinergic P2Y Receptor Activator

    P1,P2-Diuridine-5'-diphosphate (Up2U) is a symmetrical dinucleoside polyphosphate that acts as a purinergic P2Y receptor activator. This compound plays a significant role in modulating cellular responses by activating purinergic signaling pathways. It is of particular interest in research areas involving neurotransmission, cellular signaling, and immune responses. P1,P2-Diuridine-5'-diphosphate can be utilized to explore the functional roles of P2Y receptors in various biological systems.
  28. P2Y1 Antagonist

    Adenosine 3'-phosphate 5'-phosphosulfate triethylamine is a selective antagonist of the P2Y1 receptor, exhibiting no activity against P2Y2, P2Y4, or P2Y6 receptors. This compound effectively inhibits ADP-induced platelet aggregation, as well as ADP-mediated shape changes and Ca2+ elevations in platelets, while not affecting ADP's inhibition of stimulated adenylate cyclase. Additionally, it serves as a co-substrate for the sulfonation of glycans and is valuable in Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays for transferring sulfonate groups.
  29. P2Y6 Receptor Agonist

    Uridine 5'-O-thiodiphosphate (UDP-β-S) is a stable analog of uridine diphosphate that selectively acts as an agonist for the P2Y6 receptor. This compound exhibits enhanced metabolic stability, making it valuable for investigating signaling pathways related to cardiovascular diseases. Its application in research provides insights into P2Y6 receptor-mediated processes, contributing to the understanding of cellular responses and potential therapeutic targets.
  30. P2Y Purinergic Receptor Agonist

    2-Methylthio-ATP (2-MeS-ATP) is an agonist of the P2Y purinergic receptor, specifically designed for adenosine nucleotide modulation. This compound demonstrates key biological activity by inhibiting the release of inflammatory mediators from macrophages in response to lipopolysaccharide (LPS) stimulation. 2-MeS-ATP is a valuable tool for research into endotoxin shock and various inflammatory disorders, providing insights into purinergic signaling and its therapeutic potential.
  31. P2Y1 Antagonist

    Adenosine 3'-phosphate 5'-phosphosulfate lithium is a selective antagonist of the P2Y1 receptor, exhibiting no activity against P2Y2, P2Y4, or P2Y6 receptors. It effectively inhibits ADP-induced platelet aggregation, as well as ADP's ability to induce shape change and Ca2+ mobilization in platelets, without affecting ADP-stimulated adenylate cyclase activity. Furthermore, this compound acts as a co-substrate for glycan sulfonation and can be utilized in Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays to facilitate the transfer of sulfonate groups.
  32. P2Y2 Agonist

    2-Thio-UTP is a selective P2Y2 agonist exhibiting an EC50 value of 50 nM. It has demonstrated the ability to reduce pro-fibrotic gene expression and protein levels of α-smooth muscle actin. This reagent is valuable for research applications related to calcific aortic valve stenosis (CAVS) and other fibrotic disorders.
  33. P2Y14 receptor agonist

    5'-UMPS (Uridine-5'-O-monophosphorothioate) acts as an agonist of the P2Y14 receptor. This compound has been shown to slightly induce growth in HeLa cells, highlighting its potential role in cellular proliferation studies. As a valuable tool in pharmacological research, 5'-UMPS may contribute to the understanding of purinergic signaling pathways and their biological implications.
  34. P2Y Receptor Antagonist

    BX 667 is a selective reversible antagonist of the P2Y12 receptor, which plays a crucial role in platelet activation and aggregation. By inhibiting this receptor, BX 667 effectively attenuates thrombosis, making it a valuable tool for research into cardiovascular diseases and thrombotic disorders. Its oral bioactivity allows for convenient application in various in vivo studies related to platelet function and vascular health.
  35. P2Y1 receptor Antagonist

    Sp-ATPαS is a competitive antagonist of the P2Y1 receptor, primarily affecting ATP-binding proteins. It effectively inhibits calcium signaling induced by ADP and demonstrates greater metabolic stability than ATP. This reagent is valuable for exploring binding interactions of metals and nucleotides in various enzymatic reactions, making it a useful tool in biochemical studies and receptor function analysis.
  36. P2Y1 Receptor Antagonist

    MRS2298 is a potent acyclic antagonist of the P2Y1 receptor, exhibiting a Ki of 29.6 nM. This compound effectively inhibits ADP-induced platelet aggregation with an IC50 of 62.8 nM and significantly diminishes Ca2+ mobilization in platelets, presenting an IC50 of 810 nM. MRS2298 serves as a valuable tool for investigating platelet function and the role of purinergic signaling in cardiovascular research.
  37. P2Y2 Receptor Agonist

    4-Thiouridine 5′-triphosphate tetrasodium is a potent agonist of the P2Y2 and P2Y4 receptors, exhibiting EC50 values of 35 nM and 350 nM, respectively. This UTP analog is suitable for various research applications, including cross-linking experiments and transcriptional complex labeling studies, making it a valuable tool for investigating purinergic signaling pathways.
  38. Acidic Dye

    Acid Blue 129 is an acidic dye with a selective antagonistic effect on the P2Y receptor in guinea pig taenia coli, demonstrating its utility in biological research related to purinergic signaling. This compound does not interact with the P2X receptor in rat vas deferens, highlighting its specificity. Additionally, Acid Blue 129 is suitable for dyeing various materials, including cotton, wool, silk, nylon, paper, and leather, making it versatile for both scientific and industrial applications.
  39. P2Y12 Antagonist

    Elinogrel potassium is a reversible, competitive antagonist of the P2Y12 receptor. This compound demonstrates significant inhibitory effects on platelet aggregation, thereby reducing thrombosis. Elinogrel potassium is utilized in research applications focused on cardiovascular diseases and thrombosis management.
  40. P2Y14R Agonist

    MRS2905 trisodium is a selective agonist for the P2Y14 receptor, exhibiting an EC50 of 0.92 nM. This compound demonstrates a lack of activity at the UDP-activated P2Y6 receptor and other P2Y receptor subtypes. MRS2905 trisodium is a valuable tool for researchers studying purinergic signaling and its implications in various biological processes and disease states.
  41. P2Y Receptor

    Meseclazone is an inhibitor of the P2Y receptor, demonstrating significant potency in the inhibition of secondary phase ADP-induced platelet aggregation. This compound exhibits anti-inflammatory, analgesic, and antipyretic properties, making it a valuable tool for research into thrombotic disorders and the broader mechanisms of inflammation and pain modulation.
  42. P2Y14R Antagonist

    MRS4738 is a potent antagonist of the P2Y14 receptor. It demonstrates significant anti-hyperallodynic and antiasthmatic effects in vivo, making it a valuable tool for studying pain mechanisms and respiratory conditions. This compound is essential for researchers investigating the role of purinergic signaling in various biological processes.
  43. Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
  44. P2Y12 antagonist

    Ticagrelor (AZD6140) is the first reversibly binding oral P2Y(12) receptor antagonist that blocks ADP-induced platelet aggregation.
  45. P2Y6 Receptor Antagonist

    MRS 2578 is a selective antagonist of P2Y6 nucleotide receptors
  46. P2Y12 receptors inhibitor

    Cangrelor Tetrasodium is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. Unlike clopidogrel (Plavix), which is a prodrug, cangrelor is an active drug not requiring metabolic conversion.
  47. Methylthioadenosine is a naturally occurring sulfur-containing nucleoside present in all mammalian tissues.
  48. P2Y12 antagonist

    Prasugrel is a thienopyridine ADP receptor (P2Y12) antagonist, used for the reduction of thrombotic cardiovascular events.
  49. P2Y1 antagonist

    BPTU is a P2Y1 antagonist. It has been shown to provide antithrombotic efficacy and reduce bleeding liability.
  50. P2Y12 receptor antagonist

    Prasugrel (PCR 4099) Maleic acid is a platelet inhibitor with IC50 value of 1.8 μM.

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