GPCR/G Protein

Items 4601-4650 of 6977

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  1. Prostaglandin Analog

    Bima SA (Bimatoprost serinol amide) is a prostaglandin analog that targets the prostaglandin receptor pathway. It exhibits significant activity in reducing intraocular pressure, making it a valuable compound for glaucoma research. This reagent can be utilized to explore therapeutic strategies for managing ocular hypertension and advancing understanding of related eye disorders.
  2. FP Receptor Agonist

    17-Phenoxy trinor prostaglandin F2α ethyl amide is a potent agonist of the Prostaglandin F2α receptor (FP receptor). This compound is primarily investigated for its efficacy in reducing intraocular pressure, making it a valuable tool in glaucoma research. Its high activity at the FP receptor suggests potential applications in studying ocular hypertension and related therapeutic strategies.
  3. PGT Inhibitor

    T26A is a highly selective inhibitor of the prostaglandin transporter (PGT), specifically targeting PGT-mediated influx of prostaglandin E2 (PGE2). By blocking PGT activity, T26A effectively elevates extracellular PGE2 levels while reducing intracellular PGE2 metabolites and slowing the metabolism of injected PGE2 in Rattus norvegicus. This compound is valuable for research focused on understanding PGT function in adult animal models without affecting PGE2 synthesis.
  4. Prostaglandin Receptor

    8-iso Prostaglandin F3α is an isoprostane generated from the free-radical peroxidation of eicosapentaenoic acid (EPA). The compound primarily interacts with prostaglandin receptors, although its overall biological activity remains largely unexplored. A notable study indicates that 8-iso PGF3α is inactive in thromboxane receptor-mediated assays, such as those evaluating human platelet shape change, in contrast to its isoform 8-iso PGF2α, which exhibits an effective concentration of 1 μM. This suggests potential avenues for investigating its role in lipid peroxidation-related processes.
  5. Prostaglandin Receptor Antagonist

    MK-7246 S enantiomer is a selective antagonist of the prostaglandin receptor CRTH2. While it exhibits reduced activity compared to its R enantiomer, it is still valuable for investigating the role of CRTH2 in various biological processes. This compound is primarily used in research applications focused on asthma, allergic responses, and other inflammation-related studies.
  6. PGF2α Receptor Antagonist

    Ebopiprant hydrochloride is a selective antagonist of the prostaglandin F2α (PGF2α) receptor, exhibiting subnanomolar affinity with a Ki of 1 nM for the human receptor. This compound effectively inhibits PGF2α-mediated signaling pathways, making it valuable for research into conditions such as glaucoma, reproductive health, and inflammation. Its selective activity allows for the exploration of PGF2α's role in various physiological and pathological processes.
  7. Prostaglandin Receptor Control

    Latanoprost tris(triethylsilyl) ether is a synthetic precursor designed for the production of Latanoprost, a selective agonist of the prostaglandin F2α (FP) receptor. This compound is utilized in research to explore the regulation of intraocular pressure and the physiological effects of prostaglandin receptor activation. Its application is significant in studies related to glaucoma and ocular hypertension treatments.
  8. prostaglandin analog

    ZK118182 Isopropyl ester is a prostaglandin analog that functions as an anti-inflammatory agent. It is utilized in research to investigate pharmacological effects related to prostaglandin signaling pathways. This compound shows potential in studies focused on pain modulation and other inflammatory conditions.
  9. Antiulcer Agent

    Enprostil is a prostaglandin E2 derivative that functions as an antiulcer agent. It effectively inhibits gastrin-stimulated gastric acid secretion and reduces pepsin secretion, making it valuable for studying gastric and duodenal ulcers. Its mechanism of action targets the protective mucus layer in the gastrointestinal tract, helping to elucidate pathways involved in ulcer formation and treatment.
  10. Prostaglandin E1

    Prostaglandin E1 isopropyl ester is an isopropyl ester derivative of prostaglandin E1, known for its enhanced penetration properties. This compound retains the biological activities of prostaglandin E1, including vasodilation and cytoprotection, making it suitable for research in cardiovascular and gastrointestinal applications. It is an important reagent for studies investigating the pharmacological effects of prostaglandins and their therapeutic potential.
  11. Thromboxane Receptor Blocker

    AH23848 hemicalcium salt is a potent and selective thromboxane receptor blocker. It is orally active and effectively inhibits platelet deposition, making it valuable for research on thromboxane-mediated pathways in cardiovascular studies. This compound is suitable for investigating the role of thromboxane receptors in various disease models and therapeutic contexts.
  12. Thromboxane Synthase Inhibitor

    Ro 23-3423 is a selective thromboxane synthase inhibitor with an IC50 of 0.33 μM for human platelet microsomal thromboxane synthase. This compound elevates plasma levels of prostaglandin F (PGF) and prostaglandin E2 (PGE2) in a dose-dependent manner, while reducing mean systemic arterial pressure and systemic vascular resistance. Ro 23-3423 serves as a valuable tool in the investigation of cardiovascular dynamics and the mechanisms underlying general anesthesia.
  13. Platelet Aggregation Inhibitor

    CRL42872 free base is a potent oral platelet aggregation inhibitor that targets the mechanisms involved in platelet activation and aggregation. It effectively modulates platelet function, making it valuable for studying various cardiovascular and thrombotic disorders. Researchers can utilize CRL42872 free base to explore its potential therapeutic applications and elucidate the role of platelet aggregation in disease mechanisms.
  14. Prostaglandin Receptor

    20-Hydroxy-PGF2α is a metabolite derived from PGF2α and acts primarily on prostaglandin receptors. This compound is known to influence various biological processes, including modulation of inflammatory responses and regulation of smooth muscle contraction. It is utilized in research exploring reproductive biology and respiratory physiology, particularly in studies involving alveolar cells and metabolic pathways linked to prostaglandins.
  15. EP2 Receptor Agonist

    Aganepag ethanediol is an agonist of the EP2 receptor, a subtype of prostaglandin receptors involved in various physiological processes. This compound exhibits significant activity in modulating intraocular pressure, making it relevant for anti-glaucoma research. Its ability to selectively activate the EP2 receptor positions it as a valuable tool in studies aimed at exploring therapeutic interventions for glaucoma and related ocular conditions.
  16. TxA2 Receptor Agonist

    SQ 26655 is an agonist of the TxA2 receptor, known to induce aggregation of human platelets. This compound plays a crucial role in studying platelet function and thrombus formation, making it valuable for research in cardiovascular biology. Its ability to mimic thromboxane A2 activity provides insights into various pathophysiological conditions associated with hemostasis and thrombosis.
  17. Prostaglandin Receptor Inhibitor

    KF 13218 is a potent and selective inhibitor of thromboxane B2 (TXB2) synthase, exhibiting an IC50 value of 5.3 ± 1.3 nM. This compound effectively modulates prostaglandin receptor activity, making it valuable for research focused on inflammatory responses and cardiovascular disease pathways. Its long-lasting inhibition of TXB2 synthesis supports investigations into therapeutic strategies for conditions associated with excessive thromboxane production.
  18. PAR-1 Antagonist

    SCH-602539 is a selective antagonist of the protease-activated receptor 1 (PAR-1). It effectively inhibits platelet aggregation induced by PAR-1-selective thrombin receptor agonists, making it a valuable tool in studying thrombotic mechanisms. SCH-602539 has demonstrated synergistic antithrombotic effects when used in conjunction with other agents such as Cangrelor, highlighting its potential applications in cardiovascular research and drug development.
  19. PAR2 Antagonist

    AZ8838 is a potent, competitive allosteric antagonist of proteinase-activated receptor 2 (PAR2), exhibiting a pKi of 6.4 for human PAR2. This non-peptide small molecule displays significant inhibitory activity, making it valuable for research investigating PAR2-related pathophysiological processes. Its oral bioavailability enhances its utility in in vivo studies focused on pain, inflammation, and other PAR2-mediated conditions.
  20. PAR1 Antagonist

    PZ-128 is a specific and reversible antagonist of protease-activated receptor-1 (PAR1), functioning as a cell-penetrating lipopeptide pepducin. By targeting the cytoplasmic surface of PAR1, PZ-128 effectively interrupts signaling to internally-located G proteins. This compound exhibits significant biological activities, including antiplatelet, anti-metastatic, anti-angiogenic, and anticancer effects, making it beneficial for research applications in cardiovascular and cancer biology.
  21. PAR1 Agonist

    TFLLR-NH2 (TFA) is a selective agonist of the Protease-Activated Receptor-1 (PAR1), exhibiting an EC50 of 1.9 μM. It effectively activates PAR1-mediated signaling pathways, making it a valuable tool for investigating thrombin-related physiological processes. This compound is suitable for research applications in vascular biology, platelet function studies, and the exploration of cardiovascular disease mechanisms.
  22. PAR4 Antagonist

    BMS-986141 is a selective antagonist of the protease-activated receptor-4 (PAR-4) that exhibits an IC50 value of 0.4 nM. This compound demonstrates strong antithrombotic properties, making it a valuable tool for research within the fields of cardiovascular disease and thrombus formation. Its oral bioavailability enhances its utility in preclinical studies aimed at understanding the role of PAR-4 in various physiological and pathological processes.
  23. PAR-1 Antagonist

    Vorapaxar sulfate is a selective antagonist of protease-activated receptor-1 (PAR-1), demonstrating competitive inhibition with a Ki value of 8.1 nM. This antiplatelet agent effectively inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner. Vorapaxar sulfate is utilized in research focused on thrombotic disorders and cardiovascular diseases, providing insights into platelet activation and aggregation pathways.
  24. PAR2 Inhibitor

    PAR-2-IN-1 is a selective inhibitor of protease-activated receptor-2 (PAR2), targeting the PAR2 signaling pathway. This compound exhibits significant anti-inflammatory and anticancer properties, making it a valuable tool in research. Its capabilities provide insights into the role of PAR2 in various biological processes and diseases, facilitating the investigation of therapeutic interventions in inflammation and cancer.
  25. PAR2 Antagonist

    GB83 is a potent antagonist of protease-activated receptor 2 (PAR2). It effectively reverses neutrophil elastase-induced synovitis and alleviates associated pain. Additionally, GB83 inhibits the impact of MET-1 supernatant on NG neurons, making it a valuable tool for research into inflammatory responses and neurobiology.
  26. PAR1 Agonist

    TFLLR-NH2 is a selective agonist of the protease-activated receptor 1 (PAR1), exhibiting an EC50 value of 1.9 μM. This compound activates PAR1, a key receptor involved in various physiological processes, including inflammation and thrombosis. TFLLR-NH2 is valuable for research applications focused on the role of PAR1 in cellular signaling pathways and its implications in cardiovascular and neurological conditions.
  27. PAR4 Antagonist

    tcY-NH2 TFA is a potent selective antagonist of the protease-activated receptor 4 (PAR4). This peptide effectively inhibits thrombin- and AY-NH2-induced platelet aggregation as well as endostatin release. tcY-NH2 TFA is valuable for research in the fields of inflammation and immunology, providing insights into platelet function and related signaling pathways.
  28. PAR4 Antagonist

    tcY-NH2 is a selective antagonist of the protease-activated receptor 4 (PAR4), functioning through modulation of thrombin action. This peptide effectively inhibits both thrombin- and AY-NH2-mediated platelet aggregation as well as endostatin release. tcY-NH2 is valuable for investigations related to inflammation and immunology, providing insights into the role of PAR4 in various physiological and pathological processes.
  29. PAR Agonist

    Protease-Activated Receptor-4 is an agonist for proteinase-activated receptor-4 (PAR4). It plays a crucial role in mediating platelet activation and inflammatory responses. This compound is valuable for research in cardiovascular diseases and the study of thrombo-inflammatory processes.
  30. PAR Antagonist

    ML354 is a selective antagonist of the protease-activated receptor 4 (PAR4), exhibiting an IC50 of 140 nM. This compound effectively inhibits PAR4 signaling, making it valuable for research into coagulation, inflammation, and thrombosis. ML354's specificity for PAR4 offers potential applications in studying the receptor's role in various physiological and pathological processes.
  31. PAR Agonist

    VKGILS-NH2 is a reversed amino acid sequence designed as a control peptide for SLIGKV-NH2, a known protease-activated receptor 2 (PAR2) agonist. This compound serves as a valuable tool in studies investigating PAR2 signaling pathways, while demonstrating no impact on DNA synthesis in cellular assays. Its application facilitates the exploration of receptor-specific functions and contributes to a deeper understanding of PAR2-related biological processes.
  32. Platelets Activator

    PAR-4 (1-6) amide (human) is an N-terminal peptide fragment of protease-activated receptor 4 (PAR4) that acts as a platelet activator. This compound induces platelet aggregation, making it valuable for research involving hemostasis and thrombosis. It serves as a useful tool in studies aimed at understanding platelet function and the signaling pathways associated with cardiovascular diseases.
  33. TRAP/ACP5 Inhibitor

    CBK289001 is an inhibitor of tartrate-resistant acid phosphatase (TRAP/ACP5). It effectively inhibits TRAP 5bMV, TRAP 5bOX, and TRAP 5aOX with IC50 values of 125 µM, 4.21 µM, and 14.2 µM, respectively. This compound is useful for studying the role of TRAP in various biological processes and may aid in the development of therapeutic strategies targeting TRAP-related pathways.
  34. Mast Cell Tryptase Inhibitor

    APC 366 TFA is an irreversible inhibitor of mast cell tryptase, a key enzyme involved in allergic responses. This reagent is instrumental in research focused on allergic diseases and related inflammatory processes. Its ability to effectively inhibit tryptase makes it a valuable tool for studying the mechanisms underlying mast cell activation and associated pathologies.
  35. PAR1 Antagonist

    FR-171113 is a specific non-peptide antagonist of the protease-activated receptor 1 (PAR1). This compound demonstrates significant antithrombotic effects by inhibiting thrombin-induced platelet aggregation, with an IC50 value of 0.29 µM. FR-171113 is valuable for research applications focused on cardiovascular diseases and platelet function studies.
  36. PAR4 Antagonist

    PAR4 Antagonist 5 is a selective inhibitor of the protease-activated receptor 4 (PAR4) that exhibits an IC50 of less than 20 μM. This compound demonstrates significant anti-platelet aggregation activity, making it a valuable tool for investigating thrombotic diseases. Its utility in research applications related to cardiovascular conditions and hemostasis offers insights into the modulation of platelet function.
  37. PAR 1 Agonist

    TRAP-5 amide is a protease-activated receptor 1 (PAR 1) agonist peptide. This compound is utilized extensively in research focusing on platelet activation and thrombotic processes due to its ability to trigger PAR 1 signaling pathways. TRAP-5 amide serves as a vital tool for investigating cardiovascular diseases and studying the molecular mechanisms underlying hemostasis and inflammation.
  38. PAR4 Inhibitor

    PAR4 Antagonist 4 is a selective inhibitor of protease-activated receptor 4 (PAR4), demonstrating potent antiplatelet activity with an IC50 of 14.2 nM. This compound exhibits enhanced metabolic stability in human liver microsomes, with a half-life (T1/2) of 42.5 minutes. PAR4 Antagonist 4 is suitable for research applications focused on hemostasis, cardiovascular disorders, and the modulation of platelet activation pathways.
  39. Protease-Activated Receptor 4 Antagonist

    PAR4 Antagonist 1 is a potent antagonist of Protease-Activated Receptor 4 (PAR4), exhibiting an IC50 of 1.8 nM. It effectively inhibits γ-thrombin-activated PAR4 in platelet-rich plasma with an IC50 of 2 nM. This compound is suitable for research applications focused on antithrombotic mechanisms and the modulation of platelet activation pathways.
  40. PAR-1 Agonist

    Parstatin (mouse) is a cell-penetrating peptide that acts as an agonist for the protease-activated receptor 1 (PAR-1). This compound has been shown to effectively inhibit angiogenesis, making it a valuable tool in the study of vascular biology and related diseases. Its ability to modulate PAR-1 activity positions it for research applications in cancer, wound healing, and other angiogenesis-related conditions.
  41. Protease Activated Receptor (PAR)

    PAR3 (1-6) is a synthetic peptide that functions as an agonist for the protease-activated receptor (PAR1). This peptide corresponds to the first six residues of the amino-terminal tethered ligand sequence from human PAR3 and residues 39-44 from the full-length human sequence. PAR3 (1-6) effectively activates p42/44 MAPK signaling pathways in fibroblasts that express PAR1, an activation that can be inhibited by the PAR1 antagonist RWJ 56110. This reagent is valuable for research involving receptor signaling mechanisms and cellular responses to proteolytic activation.
  42. PAR-1 Agonist

    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a selective agonist for Protease-Activated Receptor 1 (PAR-1), distinguishing it from PAR-2. This bioactive peptide mediates the cellular effects associated with thrombin and plays a significant role in various thrombin-related cellular activities. Furthermore, PAR-1 is implicated in the regulation of thrombin-induced hepatocellular carcinoma, highlighting its relevance in tumor microenvironments characterized by coagulation factors. This compound is essential for studies focusing on PAR-1 signaling pathways and thrombin-related pathophysiology.
  43. PAR-2 Antagonist

    PAR-2 antagonist 1 is a selective antagonist of protease-activated receptor 2 (PAR2), exhibiting an inhibitory concentration IC50 value of 0.9 μM. This compound effectively blocks PAR2 signaling, which is implicated in the proliferation and migration of breast cancer cells. PAR-2 antagonist 1 is valuable for research applications focused on understanding PAR2's role in cancer biology and exploring potential therapeutic strategies for breast cancer treatment.
  44. PAR4 Inhibitor

    PAR4 antagonist 3 is a selective inhibitor of protease-activated receptor 4 (PAR4). This compound demonstrates significant antiplatelet activity, with an IC50 value of 26.1 nM, making it a valuable tool for studies related to thrombosis and platelet function. Additionally, PAR4 antagonist 3 shows improved metabolic stability in human liver microsomes, with a half-life of 97.6 minutes, enhancing its potential for in vivo applications.
  45. PAR1 Antagonist

    Q94 hydrochloride is a selective antagonist of the protease-activated receptor 1 (PAR1), with an IC50 value of 916 nM. It inhibits PAR1/Gαq interaction and signaling, effectively preventing PAR1-mediated increases in CCL2 mRNA and protein levels in a dose-dependent manner. Additionally, Q94 hydrochloride completely blocks thrombin-induced phosphorylation of ERK1/2 and MLC, making it a valuable tool for investigating PAR1-related pathways in various biological research applications.
  46. PAR-1 Antagonist

    Protease-Activated Receptor-1 Antagonist 2 is a potent oral antagonist of the protease-activated receptor-1 (PAR-1), exhibiting an IC50 value of 7 nM. This compound demonstrates favorable pharmacokinetic properties, making it an essential tool for studying cardiovascular diseases, including atherosclerosis and restenosis. Its targeted action on PAR-1 allows for in-depth exploration of its role in vascular biology and potential therapeutic interventions.
  47. PAR Agonist

    2-Furoyl-LIGRLO-amide TFA is a selective agonist for the proteinase-activated receptor 2 (PAR2), demonstrating a pD2 value of 7.0. This compound is utilized in biochemical research to study PAR2 signaling pathways and their role in various physiological processes, including inflammation and pain modulation. Its potency and selectivity make it a valuable tool for investigating the therapeutic potential of targeting PAR2 in disease models.
  48. PAR Agonist

    VKGILS-NH2 TFA is a reversed amino acid sequence control peptide targeting protease-activated receptor 2 (PAR2). This compound serves as a PAR agonist and is utilized in research to delineate receptor activity and signal transduction pathways. VKGILS-NH2 TFA exhibits no impact on DNA synthesis in cells, making it a suitable control for studies involving PAR2 activation.
  49. PAR2 Antagonist

    (R)-AZ8838 is a competitive antagonist of the human PAR2 (protease-activated receptor 2) with a pKi value of 5.2. This compound demonstrates anti-inflammatory effects, evidenced in a rat model of PAR2 agonist-induced paw edema. It is valuable for research applications focusing on inflammation, pain modulation, and receptor signaling pathways.
  50. Protease Activated Receptor (PAR) Antagonist

    BAY-386 is a potent Protease Activated Receptor-1 (PAR-1) antagonist that effectively inhibits the expression of pro-inflammatory factors such as MCP-1 and CXCL1 in human umbilical vein endothelial cells (HUVEC). This compound is valuable for research into inflammatory processes and vascular biology, providing insights into PAR-1 signaling pathways and their role in inflammation-related conditions.

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