ep2 receptor

EP2 receptor antagonist-2 (CID891729) is a compound that blocks EP2 receptor activation by PGE2 and reduces lactate dehydrogenase (LDH) release induced by N-methyl-D-aspartate (NMDA).

EP2 receptor antagonist-1 is a reversible, potent, agonist-dependent variant of the prostaglandin EP2 receptor antagonist.EP2 receptor antagonist-1 exhibits anti-inflammatory activity.

EP2 receptor agonist 4 selectively activates the EP2 receptor with an efficacy concentration (EC50) of 43 nM [1].

Prostaglandin E2 (PGE2) is a naturally occurring hormone involved in various physiological processes, such as smooth muscle contraction and relaxation, vasodilation and constriction, blood pressure regulation, and inflammatory regulation.

Camonagrel is a compound with inhibitory effects on Prostaglandin E2 (PGE2).

Aganepag, a potent Prostanoid EP2 receptor agonist, exhibits remarkable selectivity with an EC50 of 0.19 nM, demonstrating no activity at the EP4 receptor. Its applications are primarily in the fields of wound healing, scar reduction, scar prevention, and the treatment and prevention of wrinkles.

Omidenepag isopropyl (DE-117) is a selective prostaglandin EP2 receptor agonist and a novel topical ocular blood pressure lowering compound.Omidenepag isopropyl has a weak affinity for EP1, EP2, and FP receptors.Omidenepag isopropyl is used in studies of glaucoma and hypertension. Omidenepag isopropyl can be used to study glaucoma and hypertension.

PF-04418948 is a potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. Inhibits PGE2-induced increases in intracellular cAMP; reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM).

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.

ETHYL 2-AMINO-4-METHYL-5-PHENYLTHIOPHENE-3-CARBOXYLATE targets the prostaglandin E2 receptor EP2 subtype (human)

Treprostinil diethanolamine (UT-15C) is a potent agonist of EP2, DP1, and IP, with values of 3.6, 4.4, and 32.1 nM for EP2, DP1, and IP, respectively, and 212, 826, 2505, and 4680 nM for EP1, EP4, EP3, and FPKi, respectively. Treprostinil diethanolamine contributes to the upregulation of cAMP, maintaining vascular homeostasis and causing vasodilation in human pulmonary arteries.

Evatanepag (CP-533536 free acid) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

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,

The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors). In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively. KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells. KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.

16,16-Dimethyl prostaglandin E2 is an orally active vertebrate Hematopoietic stem cells homeostasis critical regulator. It can act through EP2 EP4 and has an interaction with the Wnt pathway.

AH 6809 is an antagonist of EP and DP receptors, with Ki values of 1217, 1150, 1597, and 1415 nM for the cloned human EP1, EP2, EP3-III, and DP receptors, respectively, and a Ki of 350 nM for the mouse EP2 receptor.

Butaprost is a chemical compound that functions as a selective agonist for the prostaglandin E receptor (EP2). It exhibits an EC50 of 33 nM and a Ki of 2.4 μM when interacting with the murine EP2 receptor. However, Butaprost demonstrates lower activity against murine EP1, EP3, and EP4 receptors. Furthermore, it effectively attenuates fibrosis by inhibiting the TGF-β/Smad2 signaling pathway [1] [2] [3].

TG11-77 HCl is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 HCl has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma half-life of 2.4 h in mice. TG11-77 HCl are representative second generation EP2 antagonists with improved pharmacodynamic and pharmacokinetic properties.

TG11-77 free base is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 free base has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma half-life of 2.4 h in mice. TG11-77 free base are representative second generation EP2 antagonists with improved pharmacodynamic and pharmacokinetic properties.

Treprostinil Sodium (UT-15) is a potent DP1, IP and EP2 agonist (EC50: 0.6 1.9 6.2 nM).

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.

19(R)-hydroxy Prostaglandin E2 (19(R)-hydroxy PGE2), present in the semen of primates, including humans, acts as a potent smooth muscle relaxant and is a selective agonist for the EP2 receptor. It exhibits an EC50 value of 200 nM for relaxing cat tracheal rings that express EP2 receptors.

Evatanepag, also known as CP-533536, is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

EP4 receptor agonist 2 (compound 31) is a potent EP4 receptor agonist, demonstrating an EC50 value of 0.8 nM and K_i values of >100,000, 38,000, and 3.1 nM for the EP2, EP3, and EP4 receptors, respectively [1].