GPCR/G Protein

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  1. BLT2 Antagonist

    BLT2 antagonist-1 is a selective antagonist of the BLT2 receptor, demonstrated to inhibit the chemotaxis of CHO-BLT2 cells with an IC50 of 224 nM, while showing no effect on CHO-BLT1 cells. It also effectively inhibits the binding of leukotriene B4 (LTB4) to the BLT2 receptor, with a Ki value of 132 nM. This compound is valuable for research into inflammatory airway diseases, including asthma and chronic obstructive pulmonary disease (COPD).
  2. Antiallergy Agent

    Sch 33303 is an orally active antiallergy agent that inhibits the release of sulfidopeptide leukotrienes, mediating its effects on inflammatory pathways. This compound demonstrates significant potential for research applications related to asthma and other allergic conditions. Its ability to modulate leukotriene signaling positions Sch 33303 as a valuable tool for investigating therapeutic strategies targeting allergic responses.
  3. Leukotriene

    Leukotriene B4-3-aminopropylamide (LTB4-APA) is an immunomodulator that targets the leukotriene pathway. It acts primarily by modulating leukotriene B4 signaling, which plays a crucial role in inflammatory responses. LTB4-APA is valuable for research applications focused on inflammation, immune response modulation, and the investigation of leukotriene-related diseases.
  4. Leukotriene Antagonist

    YM-16638 is a potent orally active leukotriene antagonist targeting leukotrienes C4, D4, and E4. It effectively inhibits their production in guinea pig trachea with IC50 values of 0.05 μM, 0.16 μM, and 0.096 μM, respectively. Additionally, YM-16638 demonstrates a dose-dependent inhibitory effect on both early and late antigen-induced respiratory responses in allergic sheep, making it a valuable tool for research in respiratory and allergic conditions.
  5. LTD4/LTE4 Antagonist

    SR2640 is a potent and selective antagonist of leukotriene D4 (LTD4) and leukotriene E4 (LTE4). It effectively inhibits LTD4-induced smooth muscle contractions in the guinea pig ileum and trachea without interfering with histamine-induced contractions. At a concentration of 23 nM, SR2640 prevents the binding of [3H] LTD4 to receptors in guinea pig lung tissue, demonstrating its high affinity. This compound is suitable for research applications related to asthma and bronchoconstriction, as it shifts the dose-response curve for LTD4-induced bronchoconstriction in guinea pigs to the right, correlating with the administered dose of SR2640.
  6. LTB4 Receptor Antagonist

    14,15-Dehydro Leukotriene B4 is a selective antagonist of the leukotriene B4 (LTB4) receptors BLT1 and BLT2, exhibiting a binding affinity with a Ki value of 27 nM for BLT1 and 473 nM for BLT2. This compound effectively inhibits LTB4-induced lysozyme release from rat polymorphonuclear leukocytes, with an IC50 of 1 µM. It is useful in studies focused on inflammation and immune response modulation.
  7. LTD4 Antagonist

    Ro 24-5913 is a potent LTD4 antagonist, exhibiting an IC50 value of 6.4 nM. This compound is primarily utilized in studies focusing on asthma, helping to elucidate the role of leukotrienes in inflammatory pathways. Its effective modulation of LTD4 activity makes it a valuable tool for researchers investigating bronchoconstriction and asthma-related conditions.
  8. CysLTR1 Antagonist

    MEN-91507 is a potent orally active antagonist of the cysteinyl leukotriene receptor 1 (CysLTR1). It effectively inhibits calcium transients induced by Leukotriene D4, exhibiting an insurmountable antagonistic behavior with a pKb of 10.25. MEN-91507 demonstrates significant efficacy in blocking Leukotriene D4-induced bronchoconstriction and microvascular leakage in guinea pig models. This compound is suitable for research applications in the fields of inflammation and immunology.
  9. Leukotriene Receptor Antagonist

    (rac)-ONO 2050297 is a potent leukotriene receptor antagonist targeting both biCysLT1 and CysLT2 receptors, with IC50 values of 17 nM and 0.87 nM, respectively. This benzoxazole derivative is valuable for studies investigating leukotriene-mediated inflammatory responses and potential therapeutic applications in conditions such as asthma and allergic reactions. Its significant antagonistic activity makes it an important tool for researchers studying leukotriene signaling pathways.
  10. LTD4 Antagonist

    Sulukast is a selective antagonist of leukotriene D4 (LTD4), which plays a critical role in bronchoconstriction. By inhibiting LTD4 activity, Sulukast effectively mitigates bronchoconstriction responses associated with this mediator. This compound is valuable in the investigation of asthma and other respiratory conditions influenced by leukotriene signaling pathways.
  11. BLT1/BLT2 Agonist

    12-epi-LTB4 is an agonist for the BLT1 and BLT2 receptors, exhibiting partial agonistic activity against both mBLT1 and mBLT2. This compound has been shown to induce phosphorylation of extracellular signal-regulated kinase in primary mouse keratinocytes, highlighting its significance in signaling pathways. It is useful for research applications focused on investigating inflammatory responses and chemotaxis in cellular models.
  12. LTB4 Receptor Antagonist

    Leukotriene B4 ethanolamide is a selective antagonist and partial agonist of the Leukotriene B4 receptor 1 (BLTR1). This compound exhibits significant anti-inflammatory activity and is shown to inhibit tumor progression associated with inflammatory processes. It serves as a valuable tool for research into the mechanisms underlying inflammation and its role in cancer biology.
  13. LTD4 antagonist

    Triptinin B is a leukotriene D4 (LTD4) antagonist isolated from the plant Tripterygium wilfordii. This compound demonstrates significant biological activity by inhibiting LTD4-mediated signaling pathways, which are implicated in various inflammatory responses. Triptinin B is useful for researching therapeutic interventions in conditions associated with leukotriene receptor activity, such as asthma and allergic responses.
  14. Leukotriene Inhibitor

    SCH 40120 is a potent leukotriene inhibitor that exhibits significant anti-inflammatory properties. This compound effectively suppresses T cell proliferation as well as both antigen-specific and polyclonal antibody responses in vitro. SCH 40120 also diminishes edematous responses and inhibits the recruitment of circulating neutrophils to inflamed tissues, making it a valuable tool in research related to anti-psoriatic agents.
  15. LTA4H Inhibitor

    JNJ-40929837 succinate is a selective and orally active inhibitor of leukotriene A4 hydrolase (LTA4H). This compound effectively inhibits aminopeptidase activity, leading to the accumulation of Pro-Gly-Pro in serum. JNJ-40929837 succinate is particularly relevant for asthma research, providing a valuable tool for investigating inflammatory pathways and potential therapeutic interventions in respiratory conditions.
  16. LTD4 Receptor Antagonist

    SC-39070 is a potent LTD4 receptor antagonist. It effectively inhibits the contractile response of leukotriene D4 (LTD4) in guinea pig trachea, making it a valuable tool for studying pathways related to allergic responses and asthma. This compound is applicable in research aimed at elucidating the roles of leukotrienes in respiratory physiology and pathology.
  17. LTB4 Analog

    SC-45694 lithium is an LTB4 analog that acts primarily as an agonist, enhancing neutrophil chemotaxis, while also functioning as an antagonist by inhibiting LTB4-induced degranulation. This dual activity makes SC-45694 lithium a valuable tool for studying inflammatory responses and the role of leukotrienes in immune regulation. Its applications in research include investigations into chemotactic mechanisms and the modulation of immune cell functions.
  18. Mast Cell Activator

    ST026567 is a potent mast cell activator that functions by inducing the secretion of prostaglandin D2 (PGD2) and leukotriene C4 (LTC4) from mast cells. This compound exhibits strong degranulation activity, making it a valuable tool for studies focused on mast cell biology and allergic responses. Research applications include investigations into inflammatory processes and the development of potential therapeutic strategies targeting mast cell-related disorders.
  19. Leukotriene Receptor Inhibitor

    (R)-Ontazolast is a potent leukotriene receptor inhibitor that effectively blocks leukotriene biosynthesis. It demonstrates a remarkable IC50 value of 0.001 µM in human polymorphonuclear leukocytes, inhibiting the release of arachidonic acid. This compound is valuable for research applications related to inflammation and immune response modulation.
  20. BLT1 Antagonist

    Moxilubant hydrochloride is a potent BLT1 antagonist that inhibits leukotriene B4 (LTB4) signaling with an IC50 of 2-4 nM. This compound demonstrates significant potential in cancer research, particularly in exploring the role of inflammatory pathways in tumor progression. Its oral activity makes it a valuable tool for studying BLT1-related mechanisms in various biological contexts.
  21. Antiasthmatic

    Zafirlukast metabolite M1 is a potent leukotriene receptor antagonist. It plays a crucial role in the management of allergic lung diseases, particularly asthma, by inhibiting the actions of leukotrienes that contribute to airway inflammation and hyperresponsiveness. This compound is useful for researching the mechanisms of asthma and evaluating therapeutic options for allergic respiratory conditions.
  22. Leukotriene B4 Inhibitor

    Chamazulene is a natural compound that acts as an inhibitor of leukotriene B4 formation. Its antioxidant properties contribute to modulating inflammatory responses, making it relevant for research in inflammation and immune response studies. Chamazulene is particularly useful in exploring pathways related to leukotriene signaling and its role in various pathologies.
  23. LTB4 Antagonist

    LTB4 antagonist 2 is a carboxamide-acid compound that functions as a selective antagonist of leukotriene B4 (LTB4), demonstrating anti-inflammatory potential. This compound exhibits a notable affinity for the LTB4 receptor, with an IC50 value of 439 nM. Its application is particularly relevant in studies exploring inflammation and related pathways in various biological systems.
  24. LTD4 Receptor Antagonist

    CP-85958 is a specific antagonist of the leukotriene D4 (LTD4) receptor. This compound exhibits significant biological activity by blocking LTD4 signaling, which is implicated in the pathophysiology of inflammatory diseases. CP-85958 is valuable in research focused on asthma and other conditions associated with leukotriene-mediated inflammation.
  25. Leukotrienes C4/D4 Antagonist

    ONO-RS-347 is a potent oral antagonist of leukotrienes C4 and D4. It effectively inhibits LTD4-induced bronchoconstriction in guinea pig models, making it a valuable tool for studying respiratory conditions. This compound holds promise for research into allergic asthma and other immediate hypersensitivity diseases, aiding in the exploration of potential therapeutic interventions.
  26. LTB4 Antagonist

    LTB4 antagonist 3 is a potent leukotriene B4 (LTB4) antagonist, exhibiting an IC50 value of 477 nM. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research into inflammatory pathways and the modulation of immune responses. It is suitable for studies focused on conditions where LTB4 plays a detrimental role, providing insights into therapeutic interventions.
  27. (5S,6R)-DiHETE Isomer

    (5S,6R)-DiHETEs is the isomer of (5S,6R)-DiHETE, targeting leukotriene receptors, particularly LTD4 receptors. It demonstrates significant biological activity by inducing contraction in guinea pig isolated ileum, with an EC50 value of 1.3 μM. This action can be effectively inhibited by LTD4 receptor antagonists, making (5S,6R)-DiHETEs valuable for research in inflammatory response and receptor signaling pathways.
  28. LTD4 Agonist

    YM-17690 is a potent agonist of leukotriene D4 (LTD4) and leukotriene E4 (LTE4), exhibiting a pKi value of 9.28 for [3H]LTD4 binding. It induces dose-dependent contractions in guinea pig ileum, lung parenchyma, and trachea, with EC50 values of 16 nM, 3.9 nM, and 22 nM, respectively. This compound is valuable for research focused on asthma, inflammation, and related respiratory conditions.
  29. Leukotriene Inhibitor

    FK-664 is a potent leukotriene inhibitor that enhances ventricular contractility and reduces the time to peak tension in cardiac cells. In canine models of heart failure, FK-664 has been shown to decrease mean circulating pressure (MCP), indicating its potential therapeutic effects. This compound is valuable for research focused on cardiovascular diseases, particularly heart failure, and its underlying mechanisms.
  30. Leukotriene B4 Receptor Antagonist

    RG 14893 is a highly potent and selective antagonist of the leukotriene B4 receptor. This compound exhibits competitive binding, demonstrating its potential to inhibit leukotriene-induced pathways. RG 14893 is valuable for research applications investigating inflammatory responses and therapeutic interventions in conditions such as asthma and other allergic reactions.
  31. LTD4 Receptor Antagonist

    Ablukast is a selective leukotriene D4 (LTD4) receptor antagonist that demonstrates significant efficacy in reducing bronchoconstriction induced by leukotriene C4 (LTC4) and antigens. This compound is valuable for research focused on allergic responses and asthma mechanisms, as it modulates the bronchial response to inflammatory mediators. It serves as an important tool in studies aiming to better understand leukotriene signaling and its impact on respiratory conditions.
  32. CYS LT1 Antagonist

    Bay-X-7195 is an antagonist of the CYS leukotriene 1 receptor (CYS LT1). It effectively mitigates bronchoconstriction induced by LTD4, demonstrating both in vitro and in vivo biological activity. This compound is valuable for research focused on allergic responses and asthma pathophysiology.
  33. LTB4 Receptor Antagonist

    SM-15178 is a selective leukotriene B4 (LTB4) receptor antagonist with an IC50 of 0.30 μM, exhibiting potent oral bioactivity. This compound effectively reduces LTB4-induced neutrophil accumulation in murine models and alleviates bronchoconstriction in guinea pig studies. SM-15178 shows significant anti-inflammatory properties and is valuable for investigating chronic inflammatory conditions, including inflammatory bowel disease, psoriasis, and asthma.
  34. Leukotriene Receptor/FLAP Inhibitor

    (S)-Veliflapon is a potent inhibitor of leukotriene biosynthesis targeting the 5-lipoxygenase activating protein (FLAP). It effectively inhibits the formation of leukotriene B4 (LTB4) in rat, mouse, and human leukocytes with IC50 values of 0.026 µM, 0.039 µM, and 0.22 µM, respectively. Additionally, (S)-Veliflapon demonstrates enantioselectivity in human whole blood, making it a valuable reagent for research in inflammation and related biological processes.
  35. LTB4 Receptor Antagonist

    SC-53228 is an orally active antagonist of the human leukotriene B4 receptor (LTB4 receptor). By specifically inhibiting this receptor, SC-53228 exerts anti-inflammatory effects primarily by reducing neutrophil infiltration. Its demonstrated efficacy and safety in various inflammatory models make SC-53228 suitable for research applications related to inflammatory diseases, including psoriasis and ulcerative colitis.
  36. Leukotriene Biosynthesis Inhibitor

    L-691678 is an inhibitor of leukotriene biosynthesis that selectively binds to the 5-lipoxygenase-activating protein (FLAP). This compound disrupts leukotriene production, making it a valuable tool for investigating leukotriene-associated pathologies, including allergic responses, asthma, and inflammatory conditions. Its ability to modulate leukotriene levels provides insights into their role in various biological processes and disease mechanisms.
  37. Leukotriene Receptor Antagonist

    SB 201146 is a potent leukotriene B4 (LTB4) receptor antagonist, exhibiting activity in the range of 10 pM to 1 μM. Its primary mechanism involves the modulation of eosinophil survival, which is a critical factor in asthma-related airway inflammation. Research indicates that SB 201146 can effectively reverse the eosinophil survival promoted by mast cells and lymphocytes, suggesting its therapeutic potential in disrupting the autocrine cysteinyl leukotriene pathway. Furthermore, this compound underscores the role of LTB4 as a paracrine mediator, influencing eosinophil dynamics in various inflammatory conditions, particularly asthma.
  38. Leukotriene Receptor Antagonist

    LY203647 is an orally active antagonist targeting the leukotriene receptors LTD4 and LTE4. This compound exhibits significant biological activity by inhibiting leukotriene-mediated signaling pathways, making it a valuable tool for research on asthma and other inflammatory diseases. LY203647 aids in the exploration of therapeutic strategies for managing conditions associated with leukotriene dysregulation.
  39. Leukotriene Receptor Antagonist

    RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that enhances peroxisomal β-oxidation and promotes peroxisome bifunctional enzymes (PBEs) in hepatocytes across various animal models. Research indicates that RG-7152 significantly elevates PBE levels and β-oxidation activity in rat and mouse liver homogenates. Furthermore, comparative in vitro studies demonstrate its ability to induce PBEs similarly to clofibric acid, highlighting its potential utility in studying peroxisome proliferation and related metabolic pathways.
  40. Leukotriene B4 Receptor Antagonist

    Ricinelaidic acid is a potent leukotriene B4 (LTB4) receptor antagonist, exhibiting a Ki of 2 μM in porcine neutrophil membranes. This compound effectively inhibits LTB4-induced chemotaxis and calcium flux in isolated human neutrophils, with IC50 values of 10 μM and 7 μM, respectively. Additionally, ricinelaidic acid demonstrates the ability to mitigate bronchoconstriction induced by LTB4 in rat models, making it a valuable reagent for studying inflammatory processes and potential therapeutic interventions in respiratory conditions.
  41. LTD4 Antagonist

    CGP-35949 sodium is a leukotriene D4 (LTD4) antagonist that exerts its effects through phospholipase inhibitory activity. It is primarily utilized in research related to asthma and other respiratory conditions, where it helps to elucidate the role of leukotrienes in inflammation and bronchoconstriction.
  42. LTD4 Antagonist

    LY290324 is a potent leukotriene D4 (LTD4) antagonist, which functions by inhibiting the action of LTD4 on its receptors. This compound effectively reduces bronchospasm induced by leukotriene C4 (LTC4), LTD4, and leukotriene E4 (LTE4). LY290324 is valuable for research exploring antigen-induced bronchospasm and related respiratory conditions.
  43. BLT2 Antagonist

    ZK-158252 is a selective antagonist of the leukotriene B4 type-2 receptor (BLT2). It exhibits inhibitory activity on leukotriene-mediated signaling pathways, making it valuable for investigating inflammatory responses. This compound is relevant for research into the modulation of immune responses and the role of BLT2 in various pathological conditions.
  44. cytokine

    Maresin conjugates in tissue regeneration 1 (MCTR1) is a potent pro-resolving cytokine that plays a critical role in reducing inflammation and promoting tissue regeneration. MCTR1 effectively antagonizes LTD4-stimulated vascular responses, making it a valuable tool for research in inflammatory diseases and tissue repair mechanisms. Its unique properties make it suitable for investigations into pro-resolving pathways and their therapeutic potential in regenerative medicine.
  45. LTD4 antagonist

    L-648051 is a leukotriene D4 receptor (LTD4) antagonist that demonstrates significant potential in modulating inflammatory responses associated with various pathological conditions. Its primary biological activity includes the inhibition of LTD4-mediated signaling pathways, which are implicated in the development of arrhythmias. This compound is valuable for research focused on cardiovascular diseases and the exploration of new therapeutic avenues for managing inflammation-related disorders.
  46. LTB4 Receptor Antagonist

    LY 292728 is a potent leukotriene B4 (LTB4) receptor antagonist. It demonstrates high affinity binding to human neutrophils with a Ki of 0.47 nM and binds even more tightly to guinea pig lung membranes with a Ki of 0.04 nM. This compound is valuable for research involving inflammation and immune response modulation, making it an important tool for studies on leukotriene signaling pathways.
  47. LTB4 Receptor Antagonist

    LY306669 is a selective antagonist of the leukotriene B4 (LTB4) receptor, demonstrating significant potency in modulating LTB4-mediated signaling. This compound is primarily utilized in research focusing on inflammatory responses and lung injury mechanisms. Its ability to inhibit LTB4 activity makes it a valuable tool for studying various pulmonary conditions and therapeutic interventions aimed at mitigating lung damage.
  48. Leukotriene A4 Hydrolase Substrate

    H-Ala-pNA is a specific substrate for leukotriene A4 hydrolase, consisting of an L-amino acid p-nitroaniline derivative. Upon catalytic hydrolysis by leukotriene A4 hydrolase, H-Ala-pNA generates p-nitroaniline, which can be quantitatively monitored at 405 nm, facilitating the assessment of enzyme activity. This compound is essential for evaluating the effectiveness of inhibitors that target the amidase function of leukotriene A4 hydrolase, contributing to research on inflammatory processes and related diseases.
  49. LTD4/PAF Antagonist

    CP-96021 hydrochloride is a potent and orally active antagonist of the leukotriene D4 (LTD4) and platelet activating factor (PAF) receptors, exhibiting Ki values of 34 nM and 37 nM, respectively. This compound demonstrates significant biological activity by blocking LTD4 and PAF signaling pathways, which are implicated in various inflammatory conditions. CP-96021 hydrochloride serves as a valuable tool for research into respiratory diseases, allergies, and other disorders mediated by these signaling molecules.
  50. Leukotriene Biosynthesis Inhibitor

    ABT-080 is an orally active inhibitor of leukotriene biosynthesis, specifically targeting the pathways responsible for the production of LTB4 and LTC4. This compound effectively prevents bronchoconstriction, making it valuable for research into asthma and related inflammatory conditions. By selectively inhibiting leukotriene synthesis without affecting PGH2 biosynthesis, ABT-080 provides a critical tool for studying the role of leukotrienes in respiratory diseases.

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