human ep1 receptor

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).

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)).

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,

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].

Prostaglandin J2 (PGJ2), a derivative of Prostaglandin D2 (PGD2), serves as a potent agonist for PGD2 receptors (DP), exhibiting affinity constants (K i) of 0.9 nM and 6.6 nM for hDP and hCRTH2 receptors, respectively. It activates cyclic AMP production with an EC50 of 1.2 nM, induces oxidative stress, neuronal apoptosis, and promotes the accumulation of ubiquitinated (Ub) proteins. Notably, PGJ2's neurotoxic properties are implicated in the progression of neurodegenerative diseases such as Alzheimer's (AD) and Parkinson's (PD) [1] [2] [3] [4].