ep1 receptor

GSK-269984A is an antagonist of Prostaglandin E2 Receptor 1 (EP1) (pIC50: 7.9).

Prostaglandin E2 (PGE2) is a natural hormone-like substance involved in various physiological functions, including the contraction and relaxation of smooth muscles, dilation and constriction of blood vessels, regulation of blood pressure, and modulation of inflammation. It can be used to induce neuropathic pain models.

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,

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

EP1-antagonist-1 (EP1 antagonist 1) is an EP1 antagonist (pKi: 7.54; pIC50: 8.5).

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.

ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist used to study diseases of the biblical system and metabolism-related diseases.

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.

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.

CJ-42794 (CJ-042794) is a selective antagonist of the prostaglandin E receptor subtype 4 (EP4), inhibiting [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5. It exhibits a binding affinity that is at least 200-fold more selective for the human EP4 receptor than for other human EP receptor subtypes (EP1, EP2, and EP3) (IC50: 8.5 (pKi)).

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.

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.

Prostaglandin K1 (compound 46) is a structurally modified prostanoid analog with an EC50 and Ki of 2800 nM for the EP1 receptor.

Prostaglandin I2 is an unstable prostaglandin compound that inhibits platelet aggregation and induces vasodilation in the pulmonary vasculature via the "I prostanoid" (IP) receptor. AFP 07, a 7,7-difluoroprostacyclin derivative, serves as a selective and potent agonist for the IP receptor (Ki=0.561 nM). It exhibits weaker affinity for EP receptors, with a Ki value of > 100 nM for EP1-3 and > 10 nM for EP4. The compound 16(R)-AFP 07 free acid is an enantiomer of AFP 07. Its biological properties, particularly those involving IP and EP receptors, are yet to be fully assessed.

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

ONO-8711 is a potent and selective competitive antagonist of the EP1 receptor, with Ki values of 0.6 nM for human EP1 and 1.7 nM for mouse EP1. It effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer [1].

SC 19220 is a prostaglandin E2 receptor EP1 antagonist.SC 19220 inhibits RANKL-induced osteoclastogenesis by inhibiting the RANK/RANKL signaling pathway in osteoclast precursors.

SC 51089 is a selective prostaglandin receptor PGE2 antagonist with selectivity for prostaglandin receptor subtypes and antinociceptive activity that improves motor deficits and rescues memory decline in the Huntington's disease R6/1 mouse model .

SC 51322 is an EP1 prostanoid receptor antagonist.

EP3 and EP1 receptor agonist

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].

GSK-269984B is a novel antagonist of EP1 receptor.

GW848687X, a potent and selective prostaglandin EP1 receptor antagonist, is used for the treatment of inflammatory pain.