GPCR/G Protein

Items 4701-4750 of 6966

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  1. IP Receptor Agonist

    MRE-269-d7 is a deuterium-labeled derivative of MRE-269, which serves as an active metabolite of selexipag. This compound functions as a selective agonist of the IP receptor, playing a critical role in research related to pulmonary arterial hypertension and vascular biology. Its unique properties make it suitable for studies investigating the modulation of prostacyclin pathways and their physiological effects.
  2. Stereoisomer

    16(S)-Iloprost is a stereoisomer of Iloprost, primarily acting as a potent inhibitor of platelet aggregation. It demonstrates significant biological activity with an IC50 value of 3.5 nM, indicating its effectiveness in reducing platelet aggregation. Additionally, it exhibits balanced binding to platelet membrane receptors, with a dissociation constant (Kd) of 13.4 nM. This compound is utilized in research applications focusing on cardiovascular diseases and hemostatic disorders.
  3. Prostaglandin Receptor

    TASP0412098 is a potent and selective antagonist of the prostaglandin receptor CRTH2/DP2, exhibiting a high binding affinity with an IC50 of 2.1 nM and functional activity with an IC50 of 12 nM. This compound demonstrates potential anti-inflammatory effects and may be beneficial in suppressing asthma, as evidenced by its efficacy in mouse and guinea pig bronchial asthma models. TASP0412098 is a valuable tool for researchers investigating the role of prostaglandin receptors in respiratory conditions and inflammation.
  4. Partial Agonist Of IP Receptors

    Taprostene sodium is a partial agonist of prostanoid IP receptors, demonstrating a unique mechanism of action in modulating vascular and cardiac functions. This compound exhibits significant cardioprotective properties and can interact additively with Prostaglandin E2 (PGE2) and selective EP2 agonists. Taprostene sodium serves as a valuable tool in cardiovascular research, particularly in studies focused on vascular biology and cardiac health.
  5. Prostaglandin Receptor

    11-keto Fluprostenol is a structural analog of prostaglandin D2 (PGD2) designed to enhance potency and extend its half-life. This compound primarily targets the FP receptor and demonstrates significant biological activity as a potent analog of PGF2α. In addition, 11-keto Fluprostenol shows moderate binding affinity for the CRTH2/DP2 receptor, with minimal activity at the DP1 receptor. Its unique profile makes it a valuable tool for research involving prostaglandin signaling pathways and related biological processes.
  6. Thromboxane Receptor Antagonist

    Linotroban is a potent, orally active thromboxane receptor antagonist (TXRA), classified as a non-prostanoid. It demonstrates significant antiplatelet activity, making it a valuable antithrombotic agent in research applications. Linotroban is utilized in studies evaluating platelet aggregation and cardiovascular disease, contributing to a better understanding of thrombotic processes.
  7. Prostaglandin Receptor Inhibitor

    MF-592 is a potent inhibitor of the prostaglandin E2 (PGE2) receptor, demonstrating an IC50 value of 3 nM. This compound exhibits favorable pharmacokinetic properties in both rat and dog models, making it a valuable tool for research in inflammation and pain modulation. Its selective inhibition of PGE2 signaling pathways supports studies aimed at understanding various biological processes and developing therapeutic strategies for related diseases.
  8. P450 ω-Hydroxylase Inhibitor

    12(S)-Hydroxy-16-heptadecynoic acid is a mechanism-based inhibitor of cytochrome P450 ω-hydroxylase, effectively targeting this enzyme to modulate its activity. With a Ki value of 1.8 μM, it demonstrates significant inhibitory potency against prostaglandin ω-hydroxylase. This compound is valuable for research applications involving metabolic studies and the modulation of lipid biosynthesis pathways.
  9. Prostaglandin Receptor

    Lythrine is an alkaloid that targets prostaglandin receptors, demonstrating inhibition of prostaglandin synthetase with an IC50 of 469 μM. This compound is valuable for research applications focused on inflammation and pain pathways, as well as studying the role of prostaglandins in various biological processes. Its potential effects on the prostaglandin synthesis pathway make it a relevant tool for exploring therapeutic strategies in related disorders.
  10. PGHS-2 Inhibitor

    12(S)-HPEPE is a potent inhibitor of prostaglandin endoperoxide synthase-2 (PGHS-2), functioning as a lipoxygenase product. This compound demonstrates significant anti-inflammatory activity by reducing interleukin 1h (IL-1h)-induced PGHS-2 expression in human lung microvascular endothelial cells. Its utility in research includes the investigation of inflammatory processes and the modulation of PGHS-2 activity, providing valuable insights into therapeutic strategies for inflammatory diseases.
  11. Prostaglandin Receptor

    (+)-15-epi Cloprostenol is an enantiomer of cloprostenol that acts as an agonist for the prostaglandin F2α (PGF2α) receptor. While it has significantly lower activity as an FP receptor ligand compared to its counter enantiomer, 15(R)-cloprostenol, its unique structural features warrant further investigation into its biological interactions. This compound may have potential applications in research exploring the modulation of prostaglandin signaling pathways and its implications in various physiological and pathological processes.
  12. PGF1α Analog

    3-Methoxy prostaglandin F1α is a PGF1α analog that exhibits similar biological activity, influencing various physiological processes. This compound may be metabolized by naturally occurring extracellular antibiotic resistance genes (eARGs), highlighting its relevance in studies of antibiotic resistance dynamics in the gut microbiome. Its applications include the investigation of prostaglandin-related pathways in gastrointestinal health and antibiotic resistance mechanisms.
  13. Ergot Derivatives

    Cianergoline is an ergot derivative primarily known for its ability to reduce intraocular pressure (IOP). Its action is mediated by the inhibition of sympathetic nervous function through interactions with both prejunctional (DA2) and postjunctional (α1) adrenergic receptors. This compound is valuable for research applications focused on glaucoma and the underlying mechanisms of ocular hypertension.
  14. Prostaglandin Receptor

    Prostaglandin K2 (PGK2) primarily targets prostaglandin receptors and is characterized as a 9,11-diketone derived from the oxidation of PGE2 or PGD2. Its biological existence remains uncertain; however, PGK2 demonstrates resistance to metabolism by 15-hydroxy PGDH in vitro. This unique stability may facilitate research into its potential roles in prostaglandin signaling and related pathways.
  15. CRTh2 Antagonist

    CRTh2 Antagonist 2 is a selective and potent CRTh2 receptor antagonist, exhibiting an IC50 of ≤10 nM. This compound is primarily utilized in research related to androgenic alopecia, offering valuable insights into the modulation of hair growth and related pathways. Its high specificity makes it an essential tool for investigating the therapeutic potential in hair loss disorders.
  16. TXA/PG-END Receptor Antagonist

    L-641953 is a selective antagonist of the thromboxane-prostaglandin endoperoxide receptor (TXA/PG-END). It effectively inhibits bronchoconstriction induced by arachidonic acid, showcasing its potential in respiratory physiology studies. This compound is particularly relevant for research in cardiovascular diseases, offering insights into the modulation of vascular responses and inflammation.
  17. Prostaglandin Analogue

    5-trans-Fluprostenol is a synthetic prostaglandin analogue that acts on the prostaglandin receptors. It exhibits significant biological activity in modulating vascular function and influencing smooth muscle contraction. This compound is utilized in research applications related to cardiovascular physiology and reproductive health studies, providing insights into prostaglandin signaling pathways.
  18. Eyelash Enhancing Agent

    Tafluprost ethyl amide is a prostaglandin derivative primarily known for its role as an eyelash enhancing agent. It effectively reduces intraocular pressure (IOP) and promotes eyelash growth, making it useful in the development of antiglaucoma ophthalmic formulations. This compound is valuable for researchers investigating treatments for ocular conditions and cosmetic applications related to eyelash enhancement.
  19. FP Receptor Agonist

    N-Cyclopropyl methyl bimatoprost is a potent agonist of the Prostaglandin F2α Receptor (FP receptor). This compound has demonstrated significant biological activity in reducing intraocular pressure, making it a valuable reagent in glaucoma research. Its mechanism of action supports the exploration of therapeutic strategies for managing ocular hypertension and related conditions.
  20. EP Receptor Agonist

    9-Keto Travoprost is an EP receptor agonist, functioning primarily through the stimulation of prostaglandin E receptors. This compound is valuable for investigating endocrine-related mechanisms and has potential applications in research focused on ocular health and intraocular pressure regulation. Its ability to selectively engage EP receptors makes it a useful tool for studying pharmacological responses in various biological contexts.
  21. Thromboxane A2 Receptor Antagonist

    Vapiprost is a thromboxane A2 receptor (TXA2 receptor) antagonist that effectively inhibits thromboxane-mediated platelet aggregation and ATP release. It demonstrates a potent inhibitory effect on the aggregation induced by U-46619, collagen, or arachidonic acid (AA) with an IC50 of less than 2.1×10^-8 M. Vapiprost is utilized in research applications focused on cardiovascular studies and platelet function, contributing valuable insights into thromboxane signaling pathways.
  22. Prostaglandin Receptor Antagonist

    CRTH2-IN-1 is a selective antagonist of the prostaglandin D2 receptor, also known as CRTH2, with an IC50 value of 6 nM in human DP2 binding assays. This compound is utilized in research focused on elucidating the role of DP2 in various biological pathways, including inflammation and immune response. Its properties make it a valuable tool for investigating therapeutic strategies in conditions associated with prostaglandin signaling.
  23. Prostaglandin Analog

    16(R)-AFP 07 free acid is a potent prostaglandin analog targeting the IP receptor, which is critical for inhibiting platelet aggregation and promoting vasodilation in the pulmonary vascular system. As a 7,7-difluoroprostacyclin derivative, it exhibits high selectivity and potency for the IP receptor (Ki = 0.561 nM). While its affinity for EP receptors is significantly lower, with Ki values exceeding 100 nM for EP1-3 and >10 nM for EP4, the full extent of 16(R)-AFP 07's biological activity, particularly at the IP and EP receptors, warrants further investigation. This compound is relevant for studies exploring vascular functions and anti-thrombotic applications.
  24. Prostaglandin Receptor Antagonist

    (S)-AL-8810 is a potent and selective antagonist of the prostaglandin F (FP) receptor, characterized as an 11β-fluoro analog of PGF2α. This compound is the C-15 epimer of AL-8810, possessing the (S) or "natural" configuration at C-15. (S)-AL-8810 is primarily utilized in research involving reproductive biology and pharmacology, offering insights into the modulation of prostaglandin signaling pathways.
  25. EP4 Receptor Antagonist

    ONO-AE3-208 sodium salt is a selective antagonist of the EP4 receptor, exhibiting a Ki value of 1.3 nM, which demonstrates its strong binding affinity. This compound has minimal effect on EP3, FP, and TP receptors, with Ki values of 30 nM, 790 nM, and 2400 nM, respectively. ONO-AE3-208 sodium salt has shown significant biological activity in inhibiting cell invasion, migration, and metastasis in prostate cancer research applications.
  26. Prostaglandin Receptor

    17-Trifluoromethylphenyl trinor Prostaglandin F2α is a potent agonist of the prostaglandin FP receptor, known for its significant biological activity as a luteolytic agent. This compound features a trifluoromethyl-substituted aromatic ring structure, akin to the phenoxy ring of travoprost, contributing to its efficacy in lowering intraocular pressure. Its pharmacological profile suggests potential applications in the treatment of glaucoma and other conditions where modulation of prostaglandin pathways is beneficial. Its luteolytic potency is comparable to or surpasses that of established agents such as fluprostenol and cloprostenol.
  27. TP receptor antagonist

    TP receptor antagonist-1 is a selective antagonist of the thromboxane A2 receptor (TP receptor), exhibiting IC50 values of 9.46 μM for TPa and 8.49 μM for TPb. This compound plays a significant role in modulating thromboxane-related signaling pathways, making it valuable for investigating cardiovascular diseases. Researchers can utilize TP receptor antagonist-1 to explore therapeutic strategies targeting TP receptor-mediated effects in various cardiovascular conditions.
  28. Metabolite

    O-Desmethyl-N-deschlorobenzoyl Indomethacin is a metabolite of the non-steroidal anti-inflammatory drug indomethacin, acting as a cyclooxygenase (COX) inhibitor. This compound demonstrates significant biological activity by reducing the viability of HL-60 leukemia cells in the presence of glucose oxidase at a concentration of 600 μM. It serves as a valuable reagent in research focused on synthesizing prostaglandin D2 receptor antagonists and elucidating the metabolic pathways of NSAIDs.
  29. PGD2 Analog

    2,3-Dinor-11beta-prostaglandin F2alpha is a key metabolite of PGD2, functioning primarily as a biomarker for elevated PGD2 levels. It is notably excreted in higher amounts in patients with mast cell activation disease (MCAD) and asthma, demonstrating a positive correlation with deteriorating lung function. This compound serves as a valuable tool for researchers studying inflammatory conditions and mast cell-related pathologies.
  30. Prostaglandin Receptor Inhibitor

    (±)12-HEPE is a prostaglandin receptor inhibitor produced through the non-enzymatic oxidation of eicosapentaenoic acid (EPA), comprising equal parts of the 12(S)- and 12(R)- isomers. The 12(S) isomer primarily mediates its biological effects in mammalian systems, demonstrating significant inhibition of platelet aggregation with an IC50 of 24 μM, comparable to that of 12-HETE. Additionally, (±)12-HEPE effectively inhibits U46619-induced contraction in rat aorta, exhibiting IC50 values ranging from 8.6 to 8.8 μM, making it valuable for research in cardiovascular and inflammatory responses.
  31. Acetylation Inhibitors

    O-Acetylsalicylhydroxamic acid is an acetylation inhibitor targeting prostaglandin H2 synthase (PGHS). It effectively suppresses prostaglandin E2 (PGE2) synthesis and inhibits the cyclooxygenase activity of PGHS in vitro. The compound specifically requires the active site residue Ser-529 for its action on human PGHS-1, with the S529A mutant displaying resistance to its inactivating effects, making it a valuable tool for research in inflammation and pain pathways.
  32. Prostaglandin Receptor

    Carboprost methyl is a methyl ester derivative of 15(S)-15-methyl Prostaglandin F2α, targeting prostaglandin receptors. This compound exhibits enhanced membrane permeability and, upon hydrolysis in vivo, releases the active form 15(S)-15-methyl PGF2α. It serves as a potent uterine stimulant and is utilized in research applications related to reproductive biology and obstetrics.
  33. Prostaglandin Receptor Antagonist

    AM211 sodium is a selective and potent antagonist of the prostaglandin D2 receptor type 2 (DP2), exhibiting an IC50 of 4.9 nM for human DP2 and similar efficacy in mouse, guinea pig, and rat models with IC50s of 7.8 nM, 4.9 nM, and 10.4 nM, respectively. Its oral bioavailability makes it an important tool for studying the role of DP2 in various biological processes, including inflammation and allergic responses. AM211 sodium is suitable for research applications investigating the modulation of prostaglandin signaling pathways.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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