Neuronal Signaling

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  1. 5-LO/COX Inhibitor

    BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) enzymes, exhibiting an IC50 of 5 μM for 5-LO. It also demonstrates inhibitory activity against COX-1 and COX-2, with IC50 values of 0.65 and 1.2 μg/mL, respectively. This compound is valuable for research applications involving inflammation and other related pathways. Its ability to concurrently inhibit key lipid mediators makes BW 755C a useful tool in studies focused on arachidonic acid metabolism and signaling pathways.
  2. COX-2 Inhibitor

    Enflicoxib is a selective inhibitor of cyclooxygenase-2 (COX-2), a key enzyme in the inflammatory pathway. This nonsteroidal anti-inflammatory compound exhibits notable anti-inflammatory, analgesic, and antipyretic effects in various animal models. Enflicoxib is valuable for research investigating COX-2-mediated processes and potential therapeutic applications in pain management and inflammation.
  3. COX-1 Inhibitor

    CP-74006 is a selective inhibitor of Cyclooxygenase-1 (COX-1). This compound demonstrates significant anti-inflammatory activity by blocking the conversion of arachidonic acid to prostaglandins, key mediators in the inflammatory response. CP-74006 is utilized in research focusing on inflammation, pain management, and cardiovascular disease, providing valuable insights into COX-1 related biological processes.
  4. COX inhibitor

    2-Chloro-N-(2,6-dimethylphenyl)acetamide is a cyclooxygenase (COX) inhibitor that modulates inflammatory responses by inhibiting the conversion of arachidonic acid to prostaglandins. Its biological activity makes it a valuable tool in research focused on inflammation and pain pathways. This compound is utilized for studying COX-related mechanisms in various biological contexts, potentially aiding in the development of anti-inflammatory therapies.
  5. COX- 2 Inhibitor

    Ocarocoxib is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 value of 1.4 μM. By inhibiting COX-2, Ocarocoxib effectively reduces the synthesis of prostaglandins, thereby imparting significant anti-inflammatory effects. This compound is useful for research on inflammation and associated pathological conditions.
  6. COX-2/5-LOX Inhibitor

    Tebufelone is a selective dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LO). It exhibits significant anti-inflammatory, analgesic, and antipyretic properties, making it useful for research into inflammatory pathways. This compound is valuable for studying the roles of COX-2 and 5-LO in various biological processes and assessing novel therapeutic strategies for inflammatory diseases.
  7. COX-1 Inhibitor

    Teriflunomide impurity 3, also known as 4-Amino-N-(4-trifluoromethylphenyl)benzamide, acts as a selective inhibitor of cyclooxygenase-1 (COX-1) with an IC50 of 30 µM. This compound exhibits significantly lower activity against COX-2, with an IC50 greater than 100 µM. Teriflunomide impurity 3 is valuable for research applications exploring inflammatory pathways and the role of COX-1 in various biological processes.
  8. COX

    ASP6537 is a selective inhibitor of recombinant human cyclooxygenase-1 (rhCOX-1), exhibiting an IC50 value of 0.703 nM. Its potent inhibition of COX-1 makes it a valuable tool for studying the role of prostaglandins in cardiovascular disease research. Researchers can utilize ASP6537 to investigate the effects of COX-1 modulation on cardiovascular pathophysiology.
  9. iNOS/COX-2 Inhibitor

    Rehmapicrogenin is a selective inhibitor of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). This compound, derived from the root of Rehmannia glutinosa, demonstrates significant anti-inflammatory properties, making it a valuable tool for research focused on inflammation pathways. Its ability to inhibit pro-inflammatory mediators such as IL-6 further underscores its relevance in studies aimed at understanding and treating inflammatory diseases.
  10. COX-1/COX-2 Inhibitor

    (S)-(+)-Ibuprofen-d3 is a deuterated analog of (S)-(+)-Ibuprofen, targeting the COX-1 and COX-2 enzymes. With IC50 values of 2.1 μM and 1.6 μM, respectively, this compound exhibits significant analgesic, anti-inflammatory, and antipyretic properties. It serves as a valuable tool for studying the pharmacodynamics and mechanisms of nonsteroidal anti-inflammatory drugs (NSAIDs) in various biological research applications.
  11. COX Inhibitor

    Isoxicam is a non-steroidal anti-inflammatory drug (NSAID) that functions as a nonselective inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). Its primary mechanism involves the inhibition of prostaglandin synthesis, making it effective in reducing inflammation and pain. Isoxicam is commonly utilized in research related to arthritis and other inflammatory conditions, providing valuable insights into the role of COX enzymes in various biological processes.
  12. COX-2 Inhibitor

    Cimicoxib is a selective COX-2 inhibitor that effectively penetrates the blood-brain barrier. It displays significant anti-inflammatory, analgesic, and antipyretic properties by inhibiting the production of thromboxane B2 and prostaglandin E2, with an IC50 of 66 nM against human COX-2. Additionally, Cimicoxib targets CYP2D15, exhibiting an IC50 of 1.6 μM in canines and 0.056 μM in felines. This compound is utilized in research involving inflammatory diseases, osteoarthritis, and perioperative pain management in orthopedic and soft tissue surgeries.
  13. COX Inhibitor

    Naproxen glucuronide, a metabolite of naproxen, functions as a non-selective cyclooxygenase (COX) inhibitor. This compound exhibits significant anti-inflammatory, analgesic, and antipyretic activity, making it useful in the study of pain relief and inflammation pathways. Research applications include examining its metabolic pathways, assessing its efficacy in various inflammatory conditions, and exploring its pharmacokinetic properties in biological systems.
  14. Dual COX/5-LOX Inhibitor

    ER-34122 is a dual inhibitor of cyclooxygenase (COX) and 5-lipoxygenase (5-LO). This compound exhibits significant anti-inflammatory activity, making it valuable for research into inflammation-related pathways. ER-34122 is particularly relevant for studies investigating the interplay between COX and 5-LO pathways in various disease models and therapeutic contexts.
  15. COX-2 Inhibitor

    Apricoxib is a selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating a potent inhibitory effect on PGE2 production with an IC50 of 1.5 nM. This compound exhibits notable biological activities, including anticancer, analgesic, and anti-inflammatory properties. Apricoxib is a valuable tool for research applications focused on inflammation, pain management, and cancer therapeutics.
  16. COX-2/PGE2 Inducer

    Rebamipide-d4 is a deuterium-labeled derivative of Rebamipide, primarily targeting cyclooxygenase-2 (COX-2). This compound induces COX-2 expression and elevates prostaglandin E2 (PGE2) levels, thereby enhancing gastric mucosal defense mechanisms in a COX-2-dependent manner. Rebamipide-d4 is utilized in various research applications focused on gastric protection and the modulation of inflammatory responses.
  17. Alkaloid

    (S)-Laudanosine is an alkaloid with a primary action on the central nervous system and cardiovascular system. It inhibits low-affinity GABA receptors, exhibiting an IC50 value of 10 μM and has the potential to induce seizures, hypotension, and bradycardia. Additionally, (S)-Laudanosine demonstrates analgesic properties through competitive binding to the opioid Mu-1 receptor, with a binding affinity characterized by a Ki value of 2.7 μM. This compound is valuable for research into neurological and cardiovascular functions.
  18. μ-Opioid Receptor Agoinst/AChE Inhibitor

    Eseroline is a potent μ-opioid receptor agonist and a selective, competitive inhibitor of acetylcholinesterase (AChE), with Ki values of 0.1 μM for AChE and 200 μM for butyrylcholinesterase (BuChE). This compound also acts as a nicotinic acetylcholine receptor allosteric enhancing ligand, enhancing acetylcholine signal transduction without directly activating the receptor. Eseroline's neurotoxic effects include cell membrane damage and energy metabolism disruption, making it a valuable tool for investigating Alzheimer's disease pathology and cholinergic signaling.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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