pgd2(dp)

PGD2-IN-1 (PGD2-inhibitor) is an effective DP receptor antagonist (IC50:0.3 nM), a compound that can inhibit prostaglandin D2 (PGD2) signaling. PGD2-IN-1 specifically targets and regulates the activity of PGD2 receptors or enzymes involved IN PGD2 synthesis or metabolism.

Laropiprant (MK-0524) is a potent and selective antagonist of prostaglandin D2 (PGD2) receptor (DP) such as and DP DP1 receptor(Ki = 0.57 nM) and TP Receptor(Ki = 2.95 nM).

CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective CRTH2 DP2 receptor antagonist. It binds to human CRTH2 DP2, DP1, and TP receptors with Ki values of 0.6, 1200, and >10,000 nM, respectively.

Elevated intraocular pressure (IOP) is an important risk factor in developing glaucoma. Certain prostaglandins such as PGF2α and PGD2, have been shown to reduce IOP. AL 6598 is the isopropyl ester prodrug of AL 6556, a PGD2 receptor agonist that binds to DP receptors with a Ki value of 3.2 μM and demonstrates an EC50 value of 0.80 μM in an in vitro functional assay. Designed to enhance corneal absorption, AL 6598 produces a maximum 53% drop in IOP of the ocular hypertensive monkey with a 1 μg dose given twice daily.

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].