Prostanoid Receptors

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  1. EP1 antagonist

    EP1-antanoist-1 is a EP1 antagonist with a pKi of 7.54 and an pIC50 of 8.5.
  2. Lipid-lowering Agent

    AZ-1355 is an effctive lipid-lowering compound, which also inhibits platelet aggregation in vivo and elevates the prostaglandin I2/thromboxane A2 ratio in vitro.
  3. CRTh2 receptor antagonist

    MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
  4. EP4 partial agonist

    GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4.
  5. DP antagonist

    PGD2-IN-1 is an antagonist of DP extracted from patent WO 2006044732 A2, example 15 (d); has an IC50 of 0.3 nM.
  6. EP2 receptor agonist

    Taprenepag isopropyl is a highly selective EP2 receptor agonist.
  7. thromboxane A2 synthase inhibitor

    Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.
  8. EP2 receptor antagonist

    TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM.
  9. prostaglandin D2 antagonist

    AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.
  10. Prostanoid EP2 receptor agonist

    Aganepag is a potent Prostanoid EP2 receptor agonist, with an EC50 of 0.19 nM, and shows no activity at EP4 receptor. Aganepag can be used in the research of wound healing, scar reduction, scar prevention and wrinkle treatment and prevention.
  11. thromboxane-prostaglandin receptor antagonist

    Terutroban is a thromboxane-prostaglandin receptor antagonist.
  12. CRTH2 antagonist

    MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5??0.5 nM.
  13. DP1/EP2 agonist

    Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6??0.1 and 6.2??1.2 nM, respectively.
  14. IP receptor agonist

    Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.
  15. PGE2 agonist

    Evatanepag (CP-533536) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.
  16. prostaglandin EP2 agonist

    AGN 210676 is a selective prostaglandin EP2 agonist extracted from patent US20070203222A1, Compound example 23, has an EC50 of 5 nM.
  17. DP1 antagonist

    L 888607 Racemate is a selective prostaglandin D2 receptor subtype 1 (DP1) antagonist, with Kis of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.
  18. PGD2 receptor type 2 (DP2) antagonist

    AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
  19. EP and DP receptor antagonist

    AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors.
  20. LTC4 inhibitor

    Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  21. EP4 antagonist

    CJ-42794 is a selective prostaglandin E receptor subtype 4 (EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3).
  22. EP1 receptor antagonist

    ONO-8130 is an orally available antagonist of EP1 receptor.
  23. EP4 antagonist

    BGC201531, also known as GTPL3380 and AP-1531, is a EP4 antagonist for the treatment of acute migraine.
  24. prostaglandin synthase inhibitor

    Pizuglanstat is a hematopoietic prostaglandin synthase inhibitor.
  25. prostanoid agonist

    QCC-374 is prostanoid agonist potentially for the treatment of pulmonary arterial hypertension.
  26. PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca2+-dependent large-conductance K+-channel in human myometrial cells.
  27. Prostaglandin Receptor Antagonist

    AL-8810 is a potent and selective antagonist of the prostaglandin F2α (PGF2α) receptor (FP receptor), with Ki values of 0.2 ± 0.06 μM in mouse 3T3 cells and 0.4 ± 0.1 μM in rat A7r5 cells. In addition to its antagonistic activity, AL-8810 also activates MAPK and ERK1/2 signaling pathways. It is commonly used in research related to elevated intraocular pressure (OHT) and primary open-angle glaucoma (POAG).
  28. Prostaglandin E2 Inhibitor

    Thielavin B is an inhibitor of prostaglandin biosynthesis, specifically targeting the synthesis of prostaglandin E2 from endoperoxide precursors. This compound demonstrates significant anti-inflammatory activity, as evidenced by its efficacy in reducing carrageenan-induced edema in rat models following intravenous administration. Thielavin B is valuable for research focused on inflammation and pain pathways.
  29. CRTH2 Receptor Antagonist

    CT-133 is a selective and potent antagonist of the CRTH2 receptor, exhibiting a Ki value of 2.2 nM, while demonstrating minimal affinity for the DP1 receptor (Ki > 3800 nM). This compound effectively inhibits neutrophil migration induced by PGD2 and has been shown to significantly reduce lung inflammation and improve lung function in a mouse model of acute lung injury (ALI) triggered by cigarette smoke. Additionally, CT-133 suppresses the overexpression of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6, and promotes the recovery of the anti-inflammatory cytokine IL-10. CT-133 is valuable for research on acute lung injury and inflammatory responses.
  30. CRTh2 Receptor Antagonist

    AZ-11665362 is a selective antagonist of the CRTh2 (DP2) receptor, exhibiting a potent IC50 of 2.6 nM. While it demonstrates slight activity towards aldose reductase and the serotonin transporter, it shows negligible inhibition of COX-1 and COX-2 enzymes. This compound is primarily utilized in research focused on asthma and other inflammatory diseases, providing valuable insights into therapeutic pathways targeting eosinophilic inflammation.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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