dp receptor

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.

AGN 210676 is a selective agonist of prostaglandin EP2(EC50 : 5 nM).

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.

AMG-009 is a selective and potent dual antagonist of CRTH2 and DP, with an IC50 value of 3 nM for CRTH2 and 12 nM for DP receptors.

BW 245C is a selective prostaglandin-like DP receptor (DP1) agonist, a prostaglandin analogue with inhibitory effects on the aggregation response of collagen, which can be used to study diseases such as stroke.

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

L-644,698 is a selective agonist of human prostanoid DP receptor.

ZK118182 isopropyl ester is a PG analog with potent DP-agonist activity (EC50 = 16.5 nM) and high affinity for the DP receptor (Ki = 74 nM).

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.

Laropiprant sodium is a potent and selective DP receptor antagonist with Ki values of 0.57 nM (TP receptors) and 2.95 nM (DP receptors).

AL-6556 is a prostaglandin DP receptor agonist.

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].

Dp[Tyr(Me)2,Arg8]-Vasopressin is a non-selective antagonist of the peptide arginine vasopressin V1b receptor [1].

AL 8810 methyl ester, a prostaglandin F(2α) analog and receptor agonist, competitively antagonizes FP receptor agonist Fluprostenol effects. It lacks significant potency against TP, DP, EP(2), EP(4) receptor subtypes in cell lines [1].

15(R)-Prostaglandin D2 functions as a DP(2) receptor (Prostaglandin Receptor) agonist with potential roles in prostatic hormone signaling and exhibits anti-inflammatory properties. It enhances actin polymerization in human eosinophils and elevates cAMP levels in platelets [1].

(R)-3-Fluoropyrrolidine hydrochloride is a derivative of fluorinated pyrrolidines. The amide series of fluorinated pyrrolidines acts as inhibitors of Dipeptidyl Peptidase (DP-IV). Novel α4β2 receptor ligands can be synthesized featuring the 3-Fluoropyrrolidine nucleus.