GPCR/G Protein

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  1. Platelet Activating Factor Antagonist

    ONO-6240 is a potent antagonist of platelet-activating factor (PAF), which plays a critical role in inflammatory responses. This compound effectively inhibits eosinophil infiltration in the airways, making it a valuable tool for researching asthma and other pulmonary conditions. Its ability to modulate PAF activity positions ONO-6240 as an important candidate for studies aimed at understanding and treating allergic and inflammatory diseases.
  2. 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.
  3. 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.
  4. PK2 Antagonist

    PKRA83 is a potent antagonist of prokineticin 2 (PK2), functioning by competing for binding sites on PKR1 and PKR2 receptors. It demonstrates significant inhibition of PK2, with IC50 values of 5.0 nM for PKR1 and 8.2 nM for PKR2. PKRA83 exhibits various biological activities, including anticancer, anti-arthritis, and anti-angiogenic effects, making it valuable for research applications in cancer biology, inflammatory diseases, and angiogenesis studies.
  5. PKR1 Antagonist

    PKR1 antagonist 1 is a selective antagonist of the PKR1 receptor, which plays a crucial role in pain signaling. This compound has demonstrated efficacy in reducing hyperalgesia and allodynia in the spared nerve injury (SNI) mouse model. Its application is significant for research focused on pain management and the underlying mechanisms of nociceptive signaling.
  6. PKR2 Antagonist

    A457 is a selective antagonist of the prokineticin receptor PKR2, exhibiting an IC50 value of 102 nM. This compound effectively restores cell surface expression and functionality of the P290S PKR2 variant, while showing no activity against the W178S and G234D PKR2 mutations. A457 is valuable for research applications focused on the modulation of PKR2-related pathways and the study of receptor mutations.
  7. TXA2 Agonist

    U-46619 is a stable analogue of Thromboxane A2 (TXA2) that functions as a potent TXA2 receptor (TP) agonist. This compound also acts as a RhoA agonist, promoting RhoA activation through TXA2 receptor engagement. U-46619 is primarily utilized in research to study thromboxane signaling and its implications in cardiovascular and inflammatory responses. Its ability to selectively activate TXA2 pathways makes it an essential tool for investigating related biological processes.
  8. Prostaglandin

    Prostaglandin D2 (PGD2) is an endogenous lipid mediator primarily involved in sleep promotion and the modulation of inflammatory responses. It is produced in various mammalian brains and is recognized for its potent ability to induce sleep and reduce inflammatory processes. PGD2 is valuable in research applications related to sleep disorders, neurobiology, and inflammation.
  9. Thromboxane-Prostaglandin Receptor Antagonist

    Terutroban sodium is a selective and orally active thromboxane-prostaglandin (TP) receptor antagonist, exhibiting an IC50 value of 16.4 nM. This compound effectively inhibits the activity of thromboxane A2 (TXA2) and prostaglandin endoperoxide receptors, demonstrating potent antithrombotic effects. Terutroban sodium also possesses anti-atherosclerotic and anti-vasoconstrictor properties, making it valuable for research applications in cardiovascular disease and related areas.
  10. PGDS Inhibitor

    2-Benzoylthiophene is a selective inhibitor of human hematopoietic prostaglandin D2 synthase (H-PGDS), exhibiting an IC50 value of 11.4 μM. This compound is valuable for investigating the role of prostaglandin D2 in inflammatory diseases and related research applications. Its inhibitory action on H-PGDS provides a useful tool for exploring therapeutic strategies targeting inflammatory pathways.
  11. EP3 Receptor Antagonist

    L-798106 is a potent and highly selective antagonist of the prostanoid EP3 receptor, exhibiting a Ki value of 0.3 nM. While it demonstrates micromolar activity at the EP4 receptor with a Ki of 916 nM, it shows minimal binding affinities at the EP1 and EP2 receptors, with Ki values exceeding 5000 nM. This compound is valuable for research applications involving the modulation of EP3 receptor-mediated pathways and investigating the role of prostanoids in various physiological processes.
  12. EP4 Receptor Agonist

    L-902688 is a potent and selective agonist of the EP4 receptor, exhibiting a Ki value of 0.38 nM and an EC50 of 0.6 nM. This compound demonstrates greater than 4,000-fold selectivity for EP4 compared to other EP and prostanoid receptors. It serves as a valuable tool for researchers investigating the role of EP4 in various biological processes and potential therapeutic applications related to inflammation and pain management.
  13. EP4 Receptor Antagonist

    L-161982 is a selective antagonist of the EP4 receptor, effectively inhibiting the biological activity of prostaglandin E2 (PGE2). It demonstrates complete blockade of PGE2-induced ERK phosphorylation and suppresses cell proliferation in HCA-7 cells. In addition, L-161982 has been shown to reduce symptoms of collagen-induced arthritis in murine models, making it a valuable tool for studying inflammatory pathways and potential therapeutic interventions in arthritis research.
  14. EP2 Receptor Agonist

    Omidenepag is a selective, non-prostanoid agonist of the EP2 receptor, exhibiting an EC50 of 1.1 nM. With an IC50 value of 10 nM for the human EP2 receptor, Omidenepag plays a crucial role in studying conditions associated with intraocular pressure. Its potent biological activity makes it a valuable tool for research into ocular diseases and related pathophysiological mechanisms.
  15. Vasodilator

    Beraprost sodium is a stable, orally active prostacyclin analog that acts as a potent vasodilator. By expanding renal blood vessels and enhancing microcirculation, it holds potential for the treatment of pulmonary arterial hypertension. Additionally, Beraprost sodium features an alkyne group, enabling its use as a click chemistry reagent that can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating various biochemical applications.
  16. EP3 Receptor Agonist

    Ricinoleic acid is a hydroxylated fatty acid and a potent agonist of the prostaglandin EP3 receptor, with an EC50 of 0.5 μM in MEG-01 cells. This compound is associated with various biological activities, including laxative effects and uterine contractions. Additionally, ricinoleic acid demonstrates both antianxiety-like and anti-inflammatory properties, making it valuable for research in pharmacology and developmental biology. Its high purity (≥99%) enhances its suitability for diverse applications, including studies related to gastrointestinal function and reproductive health.
  17. EP4 Antagonist

    EP4 receptor antagonist 1 is a highly potent and selective competitive antagonist of the prostanoid EP4 receptor, primarily utilized in cancer immunotherapy. It exhibits strong inhibition of human and mouse EP4 receptors with IC50 values of 6.1 nM and 16.2 nM, respectively, while showing minimal activity against human EP1, EP2, and EP3 receptors, with IC50s exceeding 10 μM. This specificity makes it a valuable tool for investigating the role of EP4 in various oncological processes.
  18. PGD2 receptor Agonist

    Prostaglandin J2 (PGJ2) is a potent agonist of the PGD2 receptors, notably hDP and hCRTH2, exhibiting Kis of 0.9 nM and 6.6 nM, respectively. It effectively stimulates intracellular cyclic AMP production with an EC50 of 1.2 nM. Beyond its receptor activity, Prostaglandin J2 is implicated in inducing oxidative stress, neuronal apoptosis, and the accumulation of ubiquitinated proteins. Its neurotoxic properties suggest a potential role in the pathogenesis of neurodegenerative diseases such as Alzheimer's and Parkinson's. This compound is valuable for research into receptor signaling pathways and neurodegenerative mechanisms.
  19. Prostaglandin Receptor Inhibitor

    p-Hydroxycinnamic acid is a prostaglandin receptor inhibitor that functions as a dietary phenolic compound. It demonstrates significant biological activity by inhibiting platelet activity, with IC50 values of 371 μM for thromboxane B2 production and 126 μM for lipopolysaccharide-induced prostaglandin E2 generation. This compound is often utilized in research related to inflammation, cardiovascular diseases, and platelet function studies.
  20. Prostacyclin Agonist

    ONO 1301 is a potent prostacyclin agonist that mimics the action of prostaglandin I2. It exhibits thromboxane-synthase inhibitory activity, enhancing the production of hepatocyte growth factor (HGF) from multiple cell types. Research demonstrates that ONO 1301 effectively ameliorates ischemia-induced left ventricular dysfunction in various animal models, including mouse, rat, and pig, making it a valuable tool for studies related to cardiovascular health and regenerative medicine.
  21. EP1 Antagonist

    SC-51322 is a selective antagonist of the prostaglandin E2 receptor subtype EP1, exhibiting a pA2 value of 8.1. This compound demonstrates significant analgesic properties, making it a valuable tool for research focused on pain mechanisms and inflammation. Its specificity for the EP1 receptor allows for the exploration of pathways involved in nociception and potential therapeutic interventions.
  22. EP4 Agonist

    Rivenprost is a selective agonist of the prostaglandin E receptor EP4, characterized by a Ki value of 0.7 nM. It has demonstrated hepatoprotective properties and bone anabolic activity. This compound is relevant for research in areas such as liver protection, bone metabolism, and the pharmacological modulation of EP4 receptor activity.
  23. EP2 Receptor Agonist

    Omidenepag isopropyl is a selective agonist of the EP2 receptor. Upon corneal penetration, it is converted to the active form, Omidenepag, which demonstrates high selectivity for the EP2 receptor with minimal affinity for EP1 and FP receptors. This compound is under investigation for its potential use in lowering intraocular pressure, making it a valuable candidate for glaucoma treatment research.
  24. Prostaglandin Derivative

    Thromboxane B2 is a prostaglandin derivative primarily involved in inducing arterial contraction and promoting platelet aggregation. This biological inactive product serves as a circulating catabolite of thromboxane A2, making it relevant as a diagnostic marker for angina in both peripheral venous and coronary sinus blood. Research indicates that Thromboxane B2 levels correlate with COX-1 activity inhibition in platelets. Furthermore, in preclinical models, Thromboxane B2 has demonstrated dose-dependent effects on respiratory function, producing decreases in airflow rate and dynamic lung compliance while increasing pulmonary airway resistance, highlighting its role as a bronchoactive metabolite in the arachidonic acid bioconversion pathway.
  25. 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.
  26. TXA2 Receptor Antagonist

    NTP42 is a potent thromboxane A2 (TXA2) receptor antagonist, exhibiting an IC50 of 3.278 nM in inhibiting T prostanoid receptor (TP)-mediated [Ca2+] mobilization upon stimulation with the alternative TP agonist U46619. This compound is particularly relevant for research applications targeting pulmonary arterial hypertension (PAH), offering potential therapeutic avenues for addressing this condition through TXA2 modulation.
  27. Dual Thromboxane Synthase Inhibitor and Receptor Antagonist

    Ridogrel is a dual thromboxane A2 synthase inhibitor and receptor antagonist. This compound exhibits potent antiplatelet activity, making it useful in research focused on cardiovascular diseases and thrombotic disorders. Additionally, Ridogrel displays anti-inflammatory properties, providing a valuable tool for studying inflammation-related pathways in various biological contexts.
  28. Thromboxane-prostanoid (TP) Receptor Antagonist

    SQ 29548 is a selective thromboxane-prostanoid (TP) receptor antagonist. This compound inhibits TP receptor signaling, which plays a critical role in various physiological and pathological processes, including vascular function, platelet aggregation, and inflammation. Its primary applications include research in cardiovascular diseases, thrombus formation, and the study of prostanoid biology. SQ 29548 serves as a valuable tool for investigating the therapeutic potential of modulating TP receptor activity.
  29. EP4 Antagonist

    MF-766 is a potent and selective EP4 antagonist, exhibiting a Ki value of 0.23 nM. It functions as a full antagonist in functional assays, displaying an IC50 of 1.4 nM, which slightly increases to 1.8 nM in the presence of 10% human serum. This reagent is valuable for research related to cancer and inflammatory diseases, facilitating the exploration of EP4 pathways in therapeutic contexts.
  30. Prostaglandin Receptor Inhibitor

    Ascorbyl tetra-2-hexyldecanoate is a lipophilic derivative of L-ascorbic acid that functions as a prostaglandin receptor inhibitor. This compound demonstrates protective effects on HaCaT keratinocytes, maintaining cell viability against UVB and oxidative stress while decreasing the production of inflammatory mediators IL-1α and prostaglandin E2 (PGE2). In vivo studies show that topical application enhances epidermal thickness, increases stratum corneum hydration, and improves skin texture, highlighting its potential for formulating skin whitening agents in cosmetic applications.
  31. EP4 Agonist

    TCS 2510 is a selective agonist of the EP4 receptor, known for its potential to modulate various biological processes. This compound exhibits significant activity in the context of metabolic diseases, making it a valuable tool for research applications aimed at understanding the underlying mechanisms of these disorders.
  32. Active Metabolite of Misoprostol

    Misoprostol acid is the active metabolite of Misoprostol, a synthetic analogue of prostaglandin E1 (PGE1). This compound is rapidly formed through de-esterification in the gastrointestinal tract following oral administration and is effective in preventing non-steroidal anti-inflammatory drug-induced gastric ulcers. Additionally, Misoprostol acid plays a significant role in obstetric applications, particularly in the induction of labor.
  33. EP3 Receptor Agonist

    Sulprostone is a potent and selective agonist of the EP3 receptor, a critical target in various physiological processes. This prostaglandin E2 (PGE2) analog exhibits antiulcer and nonsteroidal abortifacient properties. Sulprostone is relevant for research applications focused on pregnancy termination and the management of hemorrhages during delivery.
  34. Prostaglandin Receptor Agonist

    ONO-AE 248 is a selective agonist of the EP3 prostaglandin receptor, exhibiting notable cardioprotective properties. It significantly reduces myocardial infarction size by specifically targeting the EP3α receptor in murine models, with its beneficial effects occurring independently of hemodynamic changes. The protective mechanism may involve the activation of protein kinase C and the opening of K(ATP) channels, highlighting its potential utility in cardiovascular research.
  35. TxA2 Synthase/Receptor Inhibitor

    Picotamide is a dual inhibitor of thromboxane A2 (TxA2) synthase and its receptor, exhibiting significant antiplatelet activity. This compound is effective in reducing microalbuminuria and inhibiting the growth of carotid plaques, particularly in diabetic models. Picotamide is a valuable tool for investigating both acute and chronic cardiovascular diseases, aiding research into therapeutic interventions for these conditions.
  36. EP3 Antagonist

    EP3 antagonist 3 is a potent and selective antagonist of the EP3 receptor, exhibiting a pKi value of 8.3. This compound demonstrates excellent pharmacokinetic properties, making it suitable for in vivo studies. EP3 antagonist 3 is primarily utilized in research related to overactive bladder (OAB), providing valuable insights into potential therapeutic interventions.
  37. EP1 Antagonist

    SC 51089 free base acts as a selective antagonist of the prostaglandin E2 EP1 receptor, displaying inhibitory constants (Kis) of 1.3 μM for EP1, 11.2 μM for TP, 17.5 μM for EP3, and 61.1 μM for FP receptors. This compound demonstrates notable neuroprotective activity, making it valuable for research in neurobiology and inflammation studies. Its specificity towards the EP1 receptor positions SC 51089 free base as an important tool for investigating the effects of prostaglandin signaling in various biological systems.
  38. EP2 Inhibitor

    TG8-260 is a selective EP2 antagonist designed to mitigate the effects of inflammation in both central nervous system and peripheral diseases. This compound effectively reduces neuroinflammation and gliosis in the hippocampus of rats following pilocarpine-induced status epilepticus. With a plasma half-life of 2.14 hours and an oral bioavailability of 77.3%, TG8-260 also demonstrates potent inhibition of CYP450. Its ability to inhibit EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia makes it a valuable tool for investigating anti-inflammatory pathways in various animal models of peripheral inflammatory conditions.
  39. EP4 Receptor Agonist

    EP4 Receptor Agonist 2 is a potent agonist of the EP4 receptor, exhibiting an EC50 value of 0.8 nM. This compound has demonstrated selectivity with Ki values of >100,000, 38,000, and 3.1 nM for the EP2, EP3, and EP4 receptors, respectively. It is a valuable tool for studying the role of EP4 signaling in various biological processes and exploring potential therapeutic applications in inflammatory and cardiovascular diseases.
  40. TxA2/PGH2 Receptor Antagonist

    Ifetroban sodium is an orally active antagonist of the thromboxane A2 (TXA2) and prostaglandin H2 (PGH2) receptors. It exhibits significant antiplatelet activity and effectively inhibits tumor cell migration while having no impact on cell proliferation. This compound is valuable in research related to myocardial ischemia, hypertension, stroke, thrombosis, and cardiomyopathy.
  41. FP Receptor Agonist

    Tafluprost acid is a selective agonist of the prostanoid FP receptor, demonstrating high affinity with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Its binding affinity for the prostanoid EP3 receptor is significantly lower, with an IC50 of 67 nM, indicating a preferential interaction with the FP receptor. Tafluprost acid is primarily utilized in glaucoma research, making it a valuable tool for studies focused on intraocular pressure regulation and ocular pharmacology.
  42. EP3 Receptor Antagonist

    L-826266 is a selective and competitive antagonist of the EP3 receptor. This compound exhibits potent inhibition of EP3-mediated signaling, making it valuable for investigating pathways involved in convulsive disorders and other related conditions. Its targeted mechanism of action supports research into the role of prostaglandin signaling in neuroinflammation and seizure activity.
  43. EP2 Receptor Antagonist

    EP2 receptor antagonist-3 is a selective antagonist of the EP2 receptor, exhibiting an IC50 of 8 nM in human EP2 SPA assays and 50 nM in human EP2 cAMP assays. It enhances macrophage-mediated clearance of Amyloid-β plaques, making it a valuable tool for research into Alzheimer's disease and related neurodegenerative disorders. This compound can aid in understanding the role of EP2 receptors in immune response and amyloid pathology.
  44. Prostaglandin Receptor Antagonist

    BAY-6672 hydrochloride is a potent and selective antagonist of the human Prostaglandin F (FP) receptor, exhibiting an IC50 of 11 nM. This compound is primarily utilized in the research of inflammatory processes and pain modulation, making it valuable for studies in pharmacology and therapeutic development. Its selective action on FP receptors provides insights into prostaglandin signaling pathways and their implications in various pathophysiological conditions.
  45. Vasodilator

    Prostaglandin F1α is a potent vasodilator that primarily targets smooth muscle tissue. It has demonstrated the ability to induce relaxation of vascular smooth muscle, leading to reduced blood pressure. This compound is widely used in cardiovascular research to study its effects on vascular tone and the regulation of blood flow.
  46. EP2 Antagonist

    EP2 Receptor Antagonist-1 is a potent allosteric antagonist of the prostaglandin EP2 receptor, exhibiting reversible binding and agonist-dependent activity. This compound demonstrates significant anti-inflammatory effects, making it valuable for research focusing on inflammatory pathways and conditions. Its ability to selectively inhibit EP2 receptor activity positions it as a useful tool in pharmacological studies aimed at exploring novel therapeutic strategies.
  47. Prostanoid Derivative

    11β-Prostaglandin E2, a prostanoid derivative, acts as a selective inhibitor of [3H]PGE2 binding to hypothalamic membranes in rat models, exhibiting a Ki of 53.3 nM. This compound is valuable for studying the physiological roles of prostaglandins, particularly in neurobiology and endocrinology research contexts. Its ability to modulate prostaglandin signaling pathways makes it a significant tool for exploring inflammatory responses and reproductive biology.
  48. EP4 Receptor Agonist

    CAY10580 is a potent and selective agonist of the prostaglandin EP4 receptor, with a Ki value of 35 nM. This compound demonstrates significant biological activity in modulating inflammatory responses and vascular functions. CAY10580 is primarily utilized in research to investigate the role of EP4 signaling in various physiological and pathological processes, making it a valuable tool for studies in immunology and cardiovascular research.
  49. EP1/EP3 Receptor Agonist

    17-Phenyl-ω-trinor-PGE2 is an agonist for the EP1 and EP3 receptors. This compound showcases significant biological activity by inhibiting PAF-induced aggregation of human platelet-rich plasma and modulating Cyclic AMP production in response to Cicaprost. It is a valuable tool for research involving platelet function and receptor signaling pathways.
  50. Prostacyclin Receptor Antagonist

    BAY 73-1449 is a highly potent and selective antagonist of the prostacyclin receptor (IP), demonstrating an IC50 of less than 0.1 nM in cAMP assays using human HEL cells and rat dorsal root ganglion (DRG) neurons. This compound serves as a valuable tool in research aimed at elucidating the role of prostacyclin signaling in cardiovascular physiology, particularly in studies focused on blood pressure regulation.

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