Prostanoid Receptors

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

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.

Terutroban is a thromboxane-prostaglandin receptor antagonist.

MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5??0.5 nM.

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

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

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

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

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).

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

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

Pizuglanstat is a hematopoietic prostaglandin synthase inhibitor.

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.

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).

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.

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.

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.

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.

LAS191859 is a potent and selective antagonist of the CRTh2 receptor, exhibiting an IC50 value of 9.58 nM in human CRTh2 assays. This compound is primarily used in research related to chronic asthma, where it may help elucidate the role of CRTh2 in inflammatory pathways and potential therapeutic strategies. Its oral bioactivity makes it a valuable tool for investigating the modulation of immune responses associated with respiratory conditions.

CAY10471 is a selective antagonist of the prostaglandin D2 receptor CRTH2, demonstrating potent oral bioactivity. It effectively attenuates the progression of tubulointerstitial fibrosis and mitigates chronic contact hypersensitivity in animal models. This compound is valuable for research into inflammatory diseases and potential therapeutic pathways involving the CRTH2 receptor.

ARRY-502 is a potent and selective antagonist of the CRTh2 receptor, demonstrating oral bioavailability. By inhibiting PGD2-mediated Th2 inflammation, ARRY-502 effectively blocks eosinophil activation and airway hyperresponsiveness. This reagent holds significant potential for research applications focused on Th2-related asthma and related inflammatory disorders.

NVP-QAV680 is a selective antagonist of the CRTh2 receptor, exhibiting low nanomolar potency in inhibiting CRTh2-mediated activation of human eosinophils and Th2 lymphocytes. This compound demonstrates significant oral bioavailability and has shown efficacy in models of CRTh2-dependent mechanisms and allergic diseases in rats. Its properties make NVP-QAV680 a valuable tool for research in allergy and immunology.

TASP0376377 is a highly potent and selective antagonist of the CRTH2 receptor, exhibiting an IC50 of 13 nM. This compound demonstrates strong binding affinity for CRTH2, with an IC50 of 19 nM. TASP0376377 is valuable for research applications focusing on inflammatory responses and immune modulation, particularly in studies related to asthma, allergy, and other CRTH2-related pathways.

AM432 sodium is a selective antagonist of the CRTH2 receptor, also known as DP2. This compound exhibits high potency in human whole blood eosinophil assays, particularly under prolonged incubation conditions. Additionally, AM432 sodium has shown favorable pharmacokinetic profiles in canine and murine models of inflammatory diseases, making it a valuable tool for research in immunology and inflammatory pathways.

CRTh2 antagonist 3 is a potent antagonist of the chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2). This compound enhances the activity of phosphoinositide-dependent kinase-1 (PDK1) towards a short peptide substrate, exhibiting an EC50 of 2 μM and a Kd of 8.4 μM. Its potential applications include research into cardiovascular inflammation and the modulation of Th2-mediated responses.

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.