GPCR/G Protein

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  1. PAF Antagonist

    TCV-309 chloride is a highly effective antagonist of platelet-activating factor (PAF). It demonstrates specificity in inhibiting PAF-induced aggregation in both rabbit and human platelets, with IC50 values of 33 nM, 58 nM, and 27 nM for the corresponding assays. Additionally, TCV-309 chloride has exhibited potential therapeutic benefits in conditions such as anaphylactic shock, making it a valuable tool for research into PAF-related pathways and inflammatory responses.
  2. PAF Agonist

    Butanoyl PAF is a potent platelet-activating factor (PAF) agonist that retains over 10% of PAF's biological activity. This compound is found in significantly higher concentrations in oxidized low-density lipoprotein compared to enzymatically generated PAF, exceeding it by more than 100-fold. Butanoyl PAF is valuable in research applications aimed at understanding PAF-mediated signaling pathways and their roles in various physiological and pathological processes.
  3. PAF Receptor Antagonist

    α-Bulnesene is a potent PAF receptor antagonist, exhibiting an IC50 of 17.62 μM. Isolated from Pogostemon cablin, it demonstrates significant inhibitory activity against platelet-activating factor and arachidonic acid-induced platelet aggregation in rabbits. This compound is valuable for research exploring the modulation of platelet function and related inflammatory processes.
  4. PAF Antagonist

    Modipafant is a potent and selective platelet-activating factor (PAF) antagonist, known as UK-80067, and represents the (+)-enantiomer of UK-74505. This compound displays approximately double the intrinsic potency of its predecessor, making it a valuable tool in exploring PAF-related biological pathways. Modipafant is primarily utilized in research applications focused on inflammation, cardiovascular disease, and related therapeutic areas.
  5. PAF Antagonist

    CL-184005 is a potent platelet-activating factor (PAF) antagonist that effectively inhibits PAF-induced platelet aggregation, with IC50 values of 600 nM and 510 nM in human and rabbit platelet-rich plasma, respectively. This compound has demonstrated protective effects against endotoxin-induced gastrointestinal damage and hypotension in rat models. Additionally, CL-184005 shows promise in mitigating the effects of Gram-negative bacterial sepsis, making it a valuable tool for research in inflammatory and infectious disease models.
  6. PAF Antagonist

    Clotizolam is a thienobenzodiazepine derivative that acts as an antagonist of platelet-activating factor (PAF). It exhibits sedative, anxiolytic, anticonvulsant, and muscle relaxant properties, making it useful in various research applications related to anxiety and seizure disorders. This compound can be employed in studies aimed at understanding the mechanisms of PAF signaling and its implications in neurological and psychological conditions.
  7. PAFR Antagonist

    Kadsurin A is a novel lignan derived from Piper futokadsura, functioning as a platelet activating factor (PAF) receptor antagonist. It exhibits the ability to inhibit the binding of PAF to its receptor, thereby influencing various biological pathways related to inflammatory responses and cellular signaling. This compound serves as a valuable tool in research applications focused on understanding PAF-related mechanisms and exploring potential therapeutic interventions in related diseases.
  8. Platelet-activating Factor Receptor (PAFR) Antagonist

    BN52115 is a potent antagonist of the platelet-activating factor receptor (PAFR). This compound effectively reduces bronchopulmonary changes in vivo, making it valuable for studies investigating respiratory disorders. Its mechanism of action provides insights into the therapeutic potential for conditions linked to platelet-activating factor signaling.
  9. PAF Antagonist

    SDZ-62-434 free base is a potent platelet-activating factor (PAF) antagonist. It exhibits notable antiproliferative activity against various human solid tumors and hematological malignancies. This compound is relevant for research applications focusing on cancer treatment and the modulation of inflammatory responses mediated by PAF.
  10. PAFR Partial Agonist

    Hexanolamino PAF C-16 is a partial agonist of the Platelet-activating Factor Receptor (PAFR). This compound induces platelet aggregation and promotes macrophage production, while not increasing intracellular calcium levels ([Ca2+]i) in platelets, indicating distinct signaling pathways mediated by PAF receptors. It serves as a valuable tool for research into platelet function and macrophage biology, contributing to the understanding of PAF-related cellular responses.
  11. PAF Antagonist

    Epiyangambin is a competitive antagonist of the platelet activating factor (PAF) receptor, effectively inhibiting PAF-induced platelet aggregation in a dose-dependent manner. Additionally, it demonstrates antiproliferative activity against human colon cancer cells, specifically SW480 cell lines. This dual functionality makes Epiyangambin a valuable tool for research in both vascular biology and cancer studies.
  12. PAF Receptor Antagonist

    BN-50726 is a potent antagonist of the platelet-activating factor (PAF) receptor. It effectively inhibits PAF-induced biological responses, such as [3H]-serotonin release and hypotension, with an IC50 of 5.40 nM. This compound is valuable for research into PAF-mediated pathological processes, including inflammation, anaphylaxis, and hypotensive conditions.
  13. PAFR Inhibitor

    Cryptomeridiol is an inhibitor of the platelet-activating factor (PAF) receptor. It demonstrates significant melanogenesis inhibitory activity in α-MSH-stimulated B16 melanoma cells, making it a valuable tool for research into pigmentation processes and potential therapeutic applications in melanoma. Its mechanisms may contribute to a better understanding of PAF signaling in various biological contexts.
  14. PAFR Antagonist

    rel-(2R,4R)-2,4-Bis(3,4,5-trimethoxyphenyl)-1,3-dioxolane is a selective antagonist of the platelet-activating factor receptor (PAFR) with an inhibition constant (Ki) of 0.3 µM. This compound exhibits significant biological activity by blocking PAF-mediated signaling pathways. It is useful in research applications exploring inflammatory processes, cardiovascular function, and neurobiology, where PAFR modulation may provide therapeutic insights or novel intervention strategies.
  15. Platelet Aggregation Inhibitor

    Preschisanartanin O is a potent platelet aggregation inhibitor derived from Schisandra lancifolia. It effectively inhibits platelet aggregation induced by platelet-activating factor (PAF), highlighting its potential role in cardiovascular research. This compound is valuable for studies investigating thrombus formation and related pathological conditions, providing insight into therapeutic strategies for managing platelet-related disorders.
  16. PAF Antagonist

    UR-12633 is a potent platelet-activating factor (PAF) antagonist. It effectively reverses hypotension, inhibits coagulation abnormalities, and decreases vascular permeability and metabolic disorders in rodent models of endotoxic shock. This compound is valuable for studying the mechanisms and treatment strategies for endotoxic shock.
  17. Platelet Aggregation-related Pathway Inhibitor

    MKC-963 is a potent, orally active inhibitor targeting platelet aggregation-related pathways. This compound exhibits significant antithrombotic activity by disrupting platelet aggregation mechanisms. Additionally, MKC-963 induces autoinduction of CYP3A4, leading to enhanced metabolism in vivo. It is a valuable tool for research into platelet aggregation-related diseases, such as thrombosis.
  18. PAF Antagonist

    LAU-0901 is a potent PAF receptor antagonist, demonstrating significant neuroprotective properties. This compound effectively inhibits apoptosis, making it a valuable tool for research into neurodegenerative disorders and cell survival mechanisms. Its use in studies related to inflammation and cell signaling pathways highlights its potential for advancing understanding in these areas.
  19. Platelet Aggregation Inhibitor

    (R,R)-MK 287 is a potent platelet aggregation inhibitor targeting platelet-activating factor (PAF) pathways. It demonstrates strong inhibition of PAF binding to human platelets, polymorphonuclear leukocytes, and lung membranes, with Ki values of 6.1, 3.2, and 5.49 nM, respectively. (R,R)-MK 287 effectively prevents PAF-induced platelet aggregation and elastase release from PMNs, with ED50 values of 56 nM and 4.4 nM, respectively. Additionally, it reduces PAF-induced lethality in murine models and bronchospasm in guinea pigs, showcasing its potential applications in inflammatory and cardiovascular research.
  20. PAF Antagonist

    Israpafant is a highly selective and long-acting antagonist of the platelet activating factor (PAF) receptor, demonstrating potent inhibitory effects with IC50 values of 0.84 nM and 3.84 nM against PAF-induced aggregation in human and rabbit platelets, respectively. This compound has been shown to enhance both extracellular calcium influx and intracellular calcium release in prostate cancer cells. Additionally, Israpafant effectively attenuates allergic cutaneous responses, including eosinophilia, cytokine production, edema, and erythema, in murine models. These properties position Israpafant as a valuable tool for investigating PAF-related pathways and allergic reactions.
  21. Anti-PAF Agent

    1,6-Dihydro-4,7-epoxy-1-methoxy-3,4-methylenedioxy-6-oxo-3,8-lignan is a lignan derivative that acts as an anti-platelet-activating factor (PAF) agent. This compound exhibits significant inhibitory effects on PAF, a bioactive lipid involved in inflammatory processes and asthmatic responses. It is valuable in research focused on elucidating the role of PAF in inflammation and developing potential therapeutic strategies for related conditions.
  22. Arachidonic Acid Metabolism/Platelet Aggregation Inhibitor

    Rhazimine is an indole alkaloid that serves as a dual inhibitor of arachidonic acid metabolism and platelet aggregation induced by platelet activating factor. This compound demonstrates significant biological activity by modulating inflammatory pathways and inhibiting platelet aggregation, making it valuable for research in cardiovascular diseases and related pharmacological studies. Rhazimine's mechanism may provide insights into the development of therapeutic strategies targeting vascular inflammation and thrombotic conditions.
  23. Platelet-Activating Factor Antagonist

    Rocepafant is a specific antagonist of platelet-activating factor (PAF), known for its role in modulating inflammatory responses. Its inhibition of PAF activity makes Rocepafant a valuable reagent in studies related to rheumatoid arthritis and neurological conditions. This compound enables researchers to explore mechanisms of inflammation and potential therapeutic strategies in these areas.
  24. PAF Antagonist

    Homoeriodictyol 7-O-β-D-glucoside is a natural antagonist of platelet-activating factor (PAF). It effectively inhibits PAF-induced platelet aggregation in both human and rabbit models, demonstrating an IC50 value of 0.8 μM. This compound is valuable for research exploring the role of PAF in cardiovascular diseases and inflammation.
  25. platelet-activating factor antagonist

    Lexipafant is a potent platelet-activating factor (PAF) antagonist that effectively modulates inflammatory responses. It is primarily utilized in research focused on acute pancreatitis, where it helps elucidate the role of PAF in the inflammatory cascade. This compound serves as a valuable tool in studying the pathophysiology of inflammatory diseases and potential therapeutic interventions.
  26. PAFR Antagonist

    L-659,989 is a highly potent and selective antagonist of the platelet-activating factor receptor (PAFR). Its competitive inhibition of PAFR makes it a valuable tool for studying PAF-mediated biological processes. This compound is applicable in research areas including inflammation, cardiovascular diseases, and cell signaling pathways, providing insights into the role of PAF in various physiological and pathological conditions.
  27. Platelet-activating Factor Antagonist

    E-6123 is a selective platelet-activating factor (PAF) receptor antagonist. It inhibits PAF-mediated signaling pathways, which are implicated in various inflammatory responses and cardiovascular conditions. This compound is valuable for research into inflammation, thrombosis, and related pathologies, making it an essential tool for studying the role of PAF in disease mechanisms.
  28. Platelet-activating Factor Receptor (PAFR) Antagonist

    Bepafant is a specific antagonist of the platelet-activating factor receptor (PAFR) that demonstrates protective effects against anaphylactic lethality in both active and passive anaphylaxis models in mice and guinea pigs. This compound has been shown to reduce bronchoconstriction and mitigate blood pressure alterations associated with anaphylaxis. Bepafant is valuable for research focused on anaphylactic responses and the modulation of PAF-related pathways.
  29. PAF Antagonist

    SDZ-62-434 is a potent platelet-activating factor (PAF) antagonist. It exhibits significant antiproliferative activity against various human solid tumors and hematological malignancies. This compound is useful for research focused on cancer biology, inflammation, and related therapeutic applications.
  30. PAF Homolog

    2-O-Ethyl PAF C-16 is a homolog of platelet-activating factor (PAF) and acts as a competitive ligand for the platelet-activating factor receptor (PAFR). It exhibits significant inhibition of PAF receptor binding, demonstrated by an IC50 value of 21 nM against the PAF antagonist WEB 2086. This compound is useful for studying PAF-related signaling pathways and the physiological effects mediated by PAFR in various biological research applications.
  31. Platelet-activating Factor Receptor (PAFR) Inhibitor

    Dersalazine is a selective inhibitor of the platelet-activating factor receptor (PAFR), demonstrating significant intestinal anti-inflammatory properties. This compound shows potential efficacy in the treatment of ulcerative colitis, making it a valuable tool for research into inflammatory bowel diseases. Its ability to modulate PAFR-mediated signaling pathways makes Dersalazine a pertinent candidate for exploring therapeutic strategies targeting inflammation and related gastrointestinal disorders.
  32. Platelet-activating Factor Antagonist

    Ro 19-1400 is a platelet-activating factor antagonist that inhibits immunoglobulin E-dependent mediator release. This compound is effective in blocking the actions of platelet-activating factor (PAF), a phospholipid that plays a crucial role in inflammatory processes. Ro 19-1400 is primarily utilized in studies exploring allergic responses and inflammation, making it valuable for research applications aimed at understanding and developing treatments for allergies and related conditions.
  33. PAF Receptor Antagonist

    L 651142 is a weak antagonist of the platelet activating factor (PAF) receptor. This compound effectively inhibits the binding of [3H]PAF to membranes derived from rabbit platelets, human platelets, and human lung tissues, with inhibition constants (Kis) of 0.839 μM, 1.82 μM, and 3.64 μM, respectively. L 651142 is utilized in research applications that explore the role of PAF in physiological and pathological processes, making it valuable for studies related to inflammation, thrombosis, and respiratory function.
  34. Platelet-activating Factor Receptor (PAFR) Antagonist

    ABT-299 is a prodrug that functions as an antagonist of the platelet-activating factor receptor (PAFR). It demonstrates notable inhibitory activity on PAF-induced β-platelet globulin release in vitro following administration in humans, a mechanism that may involve its metabolite, pyridine-N-oxide. This compound is of particular interest for research into inflammatory responses and platelet activation processes.
  35. PAF Inhibitor

    CV 3988 is a selective inhibitor of platelet-activating factor (PAF), a lipid mediator involved in various inflammatory processes. By blocking PAF activity, CV 3988 demonstrates potential in mitigating inflammation-related pathways and may be valuable in studying conditions influenced by PAF. This compound is suitable for research applications in inflammation, cardiovascular diseases, and related areas of biochemical investigation.
  36. PAFR Inhibitor

    Piperulin A is a selective inhibitor of the platelet-activating factor receptor (PAFR). It effectively disrupts the specific binding of PAFR on isolated rabbit platelet plasma membranes, demonstrating an IC50 value of 7.3 μM. This compound is valuable for research applications focused on understanding PAFR-related signaling pathways and their implications in various physiological and pathological processes.
  37. PAF Inhibitor

    Pinusolidic acid is an inhibitor of platelet-activating factor (PAF), demonstrating an IC50 value of 23 μM. This compound is primarily utilized in research to study the roles of PAF in various biological processes and diseases, including inflammation and thrombosis. Its inhibitory properties make it a valuable tool for investigating PAF-related pathways and potential therapeutic applications.
  38. Platelet Aggregation Inhibitor

    Aggreceride A is a potent platelet aggregation inhibitor that targets multiple pathways involved in thrombosis. It exhibits significant inhibitory activity against platelet aggregation induced by Adenosine 5'-diphosphate (ADP), arachidonic acid, and platelet-activating factor (PAF), making it valuable for cardiovascular research. However, it demonstrates reduced efficacy against collagen-induced aggregation. This compound is suitable for studying mechanisms of platelet function and the effects of aggregation inhibitors in various therapeutic contexts.
  39. PAF Inhibitor

    BN 52111 is a potent platelet-activating factor (PAF) receptor antagonist. It inhibits PAF signaling, which plays a crucial role in various physiological processes, including inflammation and thrombosis. BN 52111 is primarily utilized in research applications to investigate the role of PAF in disease models and to explore potential therapeutic interventions.
  40. PAF Antagonist

    L662,025 is a potent and irreversible antagonist of the platelet-activating factor (PAF) receptor. It demonstrates a strong binding affinity with an IC50 value of 1 μM for receptor binding and effectively inhibits platelet aggregation at an IC50 value of 5.6 μM. This compound is primarily utilized in research applications focused on delineating the biological roles of PAF in various physiological and pathological processes.
  41. Platelet Aggregation Inhibitor

    Aggreceride B is a potent platelet aggregation inhibitor targeting pathways involved in thrombus formation. It effectively inhibits platelet aggregation induced by Adenosine 5'-diphosphate (ADP), arachidonic acid, and platelet activating factor (PAF), while demonstrating reduced activity against collagen-induced aggregation. This compound is valuable in studies focused on thromboembolic diseases and platelet function analysis.
  42. Antiplatelet Aggregation Agent

    Oxopurpureine is an oxoaporphine that functions as an antiplatelet aggregation agent. It effectively inhibits platelet aggregation induced by collagen, thrombin, and arachidonic acid. This compound is valuable for research applications focused on hemostasis, thrombosis, and related cardiovascular studies.
  43. PAF Antagonist

    Kadsurenin B is a potent antagonist of platelet-activating factor (PAF), exhibiting notable neuroprotective properties. This compound is of significant interest in pharmacological research due to its diverse biological activities, including antibacterial, anti-inflammatory, antioxidant, antiplatelet aggregation, cytotoxic, and antiparasitic effects. Kadsurenin B may be utilized in various applications, making it valuable for studies focused on neuroprotection and inflammation modulation.
  44. PAF Antagonist

    TCV-309 is a potent antagonist of platelet-activating factor (PAF). It demonstrates protective effects on cardiac function, particularly during ischemia-reperfusion, with significant improvement in left ventricular function observed (77.6% recovery at 1 μM). This compound is valuable for research applications involving cardiovascular disease and related ischemic conditions.
  45. PAF Receptor Antagonist

    Minopafant is a potent antagonist of the platelet-activating factor (PAF) receptor. It demonstrates significant biological activity by inhibiting PAF-mediated signaling pathways, which are implicated in various pathological conditions. This compound is primarily utilized in research focused on cerebral vasospasm, particularly following subarachnoid hemorrhage, providing insights into its therapeutic potential and underlying mechanisms.
  46. Platelet Aggregation Inhibitor

    Aggreceride C is a potent platelet aggregation inhibitor targeting multiple pathways involved in platelet activation. It effectively inhibits aggregation induced by Adenosine 5'-diphosphate (ADP), arachidonic acid, and platelet activating factor (PAF) while demonstrating reduced activity against collagen-induced aggregation. This compound is valuable for research applications focused on thrombosis and vascular biology.
  47. Platelet-activating Factor Receptor (PAFR)

    PAF-AN-1 is a selective antagonist of the platelet-activating factor receptor (PAFR). It inhibits PAF-mediated signaling pathways, demonstrating the ability to modulate inflammation and allergic responses. PAF-AN-1 is utilized in research applications focused on cardiovascular diseases, asthma, and other conditions driven by PAF activity.
  48. CRTH2/DP Receptors Dual Antagonist

    Vidupiprant is a phenylacetic acid derivative that acts as a dual antagonist of CRTH2 (DP2) and prostanoid D receptors (DP1). It exhibits high potency with IC50 values of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. This compound shows promise for therapeutic applications in asthma management and related respiratory conditions.
  49. CRTh2 Antagonist

    LAS191859 is a potent and selective antagonist of the CRTh2 receptor, exhibiting an IC50 value of 9.58 nM in human CRTh2 assays. This compound is primarily used in research related to chronic asthma, where it may help elucidate the role of CRTh2 in inflammatory pathways and potential therapeutic strategies. Its oral bioactivity makes it a valuable tool for investigating the modulation of immune responses associated with respiratory conditions.
  50. CRTH2 Antagonist

    CAY10471 is a selective antagonist of the prostaglandin D2 receptor CRTH2, demonstrating potent oral bioactivity. It effectively attenuates the progression of tubulointerstitial fibrosis and mitigates chronic contact hypersensitivity in animal models. This compound is valuable for research into inflammatory diseases and potential therapeutic pathways involving the CRTH2 receptor.

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