EP Agonist

Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with K_is of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases.

CP-432 (CP-734432) is a EP4 receptor agonist with an IC₅₀ of 2 nM for human sources, 8 nM for canine sources, and an EC₅₀ of 1 nM for human sources. CP-432 stimulates cAMP production and activates β-lactamase (β-lactamase) activity via the cAMP response element signaling pathway. CP-432 is applicable to research related to glaucoma.

L-902688 is a potent, selective and orally active EP4 receptor agonist with a K_i of 0.38 nM and an EC₅₀ of 0.6 nM. L-902688 shows >4,000-fold selective for EP4 over other EP and prostanoid receptors.

Omidenepag (UR-7276), a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC₅₀ of 1.1 nM. Omidenepag shows binding affinities (IC₅₀) 10 nM for h-EP2. Omidenepag is used in research on diseases related to intraocular pressure.

Evatanepag (CP-533536) is a non-prostanoid, potent and selective EP₂ receptor agonist. Evatanepag can induce local bone formation in vivo. Evatanepag can be used in the research of fractures, bone defects, asthma.

Prostaglandin J2 (PGJ2), an endogenous metabolite of Prostaglandin D2 (PGD2; HY-101988), is a potent PGD2 receptor (DP) agonist with K_is of 0.9 nM and 6.6 nM for hDP and hCRTH2, respectively. Prostaglandin J2 stimulates intracellular cyclic AMP production with an EC₅₀ value of 1.2 nM. Prostaglandin J2 induces oxidative stress and neuronal apoptosis. Prostaglandin J2 induces the accumulation/aggregation of ubiquitinated (Ub) proteins. Prostaglandin J2 is highly neurotoxic and potentially contributes to many neurodegenerative conditions, including Alzheimer's (AD) and Parkinson's diseases (PD).

Rivenprost (ONO-4819; ONO-AE1-734) is a selective agonist for prostaglandin E receptor EP4 with K_i of 0.7 nM. Rivenprost exhibits hepatoprotective and bone anabolic effects.

Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. Omidenepag isopropyl shows only weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as an intraocular pressure (IOP)-lowering agent.

Treprostinil (UT-15) sodium is a potent DP1 and EP2 agonist with EC₅₀ values of 0.6±0.1 and 6.2±1.2 nM, respectively.

Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers. Misoprostol is an oral agent used to induce labor.

EP4 receptor agonist 2 (compound 31) a potent EP4 receptor agonist with an EC₅₀ value of 0.8 nM; K_i values of >100000, 38000, 3.1 nM for EP2, EP3, EP4 respectively.

TCS 2510 is a selective EP4 agonist. TCS 2510 can be used for the research of metabolic diseases.

Taprenepag isopropyl is a highly selective EP₂ receptor agonist.

Sulprostone (SHB 286) is a potent and selective EP3 receptor agonist. Sulprostone (SHB 286) is a prostaglandin E2 (PGE2) analogue and has antiulcer and nonsteroidal abortifacient effects. Sulprostone has potential for the research of pregnancy termination and hemorrhages during delivery.

Tafluprost acid (AFP-172), an active metabolic form of Tafluprost, is a selective prostanoid FP receptor agonist. Tafluprost acid shows a high affinity for human prostanoid FP receptor with K_i and EC₅₀ values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC₅₀=67 nM) than for the prostanoid FP receptor. Tafluprost acid can be used in the research of glaucoma.

17-Phenyl-ω-trinor-PGE2 is a PGE2 (HY-101952) analog, which is an agonist for EP1 and EP3 receptor. 17-Phenyl-ω-trinor-PGE2 inhibits the PAF-induced aggregation of human platelet-rich plasma (PRP) and Cicaprost (HY-19583) induced Cyclic AMP (HY-B1511) production.

CAY10580 is a potent and selective prostaglandin EP₄ receptor agonist (K_i=35 nM).

Treprostinil (UT-15C) diethanolamine is a potent EP2, DP1 and IP agonist with K_i values of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1, IP, EP1, EP4, EP3 and FP, respectively. Treprostinil (UT-15C) diethanolamine increases upregulation of cAMP toward maintaining homeostasis within the vasculature. Treprostinil (UT-15C) diethanolamine can result in vasodilatation of human pulmonary arteries.

PGN-9856 is a selective and high affinity (pK_i ≥ 8.3) ligand at EP2 receptor. PGN-9856 is a potetn and non-prostanoid EP2 receptor agonist (pEC₅₀ ≥ 8.5). PGN-9856 shows anti-inflammatory and anti-glaucoma activities.

Aganepag isopropyl (AGN-210961) is an EP2 agonist.