EP4

EP4 Receptor Antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist, effective for cancer immunotherapy. It inhibits both human and mouse EP4 receptors with IC50 values of 6.1 nM and 16.2 nM, respectively, while displaying minimal activity (IC50s >10 μM) against human EP1, EP2, and EP3 receptors.

EP4-IN-1 is a potent prostaglandin EP4 receptor inhibitor with potential anti-tumor, anti-inflammatory, and analgesic activities for studying immune and tumor diseases.

EP4 receptor antagonist 3 is a highly potent and specific inhibitor of the EP4 receptor, intended for research purposes in studying EP4 receptor-mediated diseases, including acute and chronic pain, osteoarthritis, rheumatoid arthritis, and cancer.

MK-2894 is a prostaglandin receptor 4 antagonist.MK-2894 has anti-inflammatory activity and may be used in the study of inflammation.

L-161982 is a selective EP4 receptor antagonist that inhibits PGE2-induced ERK phosphorylation and cell proliferation in HCA-7 cells and alleviates collagen-induced arthritis in mice.

L-902688 is a potent, highly selective and orally active EP4 receptor agonist with a Ki value of 0.38 nM and an EC50 value of 0.6 nM. Its selectivity for the EP4 receptor is more than 4000-fold higher than that for other EP receptors and prostanoid receptors.

TP-16 is a novel potent and selective EP4 antagonist that blocks the function of IMCs and enhances cytotoxic T cell-mediated tumor elimination in vivo.

BAY-1316957 is a highly potent and selective EP4 receptor antagonist. With an IC50 of 15.3 nM. Good oral bioavailability[1].

L-798106 (CM9) is a selective and potent prostaglandin-like EP3 receptor antagonist that inhibits EP4, EP1, and EP2 receptors, suppresses levels of pro-inflammatory cytokines in atherosclerosis, and attenuates PGE2-induced cough.

Prostaglandin E1 (Alprostadil) is the naturally occurring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Prostaglandin E1 is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.

GW627368 (GW 627368X)X is a novel, potent and selective antagonist of prostanoid EP4 receptor.

TCS 2510 (CAY10598) is a selective PGE2 and EP4 receptor agonist that enhances the intracellular concentration of cAMP and the abundance of active β-caten.TCS 2510 inhibits TNF-alpha production and may be useful in the study of diseases associated with metabolic disorders.

Travoprost (Fluprostenol isopropyl ester) is used to treat glaucoma and ocular hypertension,is a potent and selective FP prostaglandin receptor agonist.

BGC201531 (AP-1531) is a EP4 antagonist for the treatment of acute migraine.

BGC-20-1531 hydrochloride(1186532-61-5 free base) (GTPL3380 hydrochloride) is a EP4 antagonist for the treatment of acute migraine.

MF-766 is a highly potent, selective, and orally active EP4 antagonist with a Ki of 0.23 nM, acting as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. It is useful for cancer and inflammation diseases research [1][2].

E7046 is a specific, orally bioavailable EP4 antagonist (IC50: 13.5 nM, Ki: 23.14 nM), exhibiting anti-tumor activities.

ONO-AE3-208 (AE 3-208) is an EP4 antagonist. It suppresses cell migration, invasion, and metastasis of prostate cancer.

Grapiprant (AAT-007) is a selective EP4 receptor antagonist. Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor (IC50: 35 nM, Ki: 24 nM).

KAG-308 is an effective selective and orally active agonist of the EP4 receptor (Ki: 2.57 nM and EC50: 17 nM for human EP4 receptor), more selective over EP1, EP2, EP3, and IP receptor. KAG-308 suppresses colitis and promotes histological mucosal healing,

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

Omidenepag (UR-7276) is a selective and potent prostaglandin E2 receptor 2 (EP2) agonist and a novel topical ocular hypotensive agent.Omidenepag is used in the study of glaucoma and hypertension.

EP4 receptor agonist 3 is an activator of the EP4 receptor and is useful for research in the DSS-induced colitis mouse model.

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, with an IC50 of 1.1 nM. This compound inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM. In RAW 264.7 macrophages, it reduces the expression of PGE2-induced IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C motif) ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase 1 (Arg1) mRNA. In the CT26 mouse colon cancer model, EP4 receptor antagonist 7, combined with an anti-PD-1 antibody, inhibits tumor growth and enhances CD8+ T cell infiltration into the tumor.