Prostaglandin D2

Prostaglandin D2 (PGD2), a major prostaglandin produced actively in the brains of various mammals, is a potent endogenous sleep-promoting substance.

15(S)-15-methyl Prostaglandin D2 (15(S)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2. Unlike PGD2, 15(S)-15-methyl PGD2 induces vasoconstriction, increases systemic blood pressure, and exhibits significantly reduced inhibitory activity on ADP-induced platelet aggregation. It also demonstrates strong antifertility activity in hamsters, being 200-fold more potent than PGD2.

Prostaglandin D2 (PGD2) is the major eicosanoid product of mast cells and is produced in large quantities by hematopoietic PGD synthase during allergic and asthmatic anaphylaxis. It causes vasodilation, flushing, hypotension, and is an inhibitor of platelet aggregation. Prostaglandin D2 methyl ester (PGD2 methyl ester) is a more lipid-soluble, cell-permeable prodrug form of PGD2. It binds to the human and mouse PGD2 receptors (DP1 and CRTH2/DP2) with 5-10 fold lower affinity than PGD2.

15(R)-15-methyl Prostaglandin D2 (15(R)15methyl PGD2) is a synthetic analogue of PGD2 and a selective and potent CRTH2/DP2 receptor agonist that modulates eosinophil CD11b expression, actin polymerisation and chemotaxis.

Prostaglandin D2 ethanolamide (PGD2-EA) is a bioactive lipid produced by the sequential metabolism of anandamide (arachidonoyl ethanolamide) by cyclooxygenase (COX) enzymes, in particular by COX-2, and PGD synthase. The biosynthesis of PGD2-EA from anandamide can also be increased when anandamide metabolism is diminished by deletion of fatty acid amide hydrolase. PGD2-EA is inactive against recombinant prostanoid receptors, including the D prostanoid receptor. It increases the frequency of miniature inhibitory postsynaptic currents in primary cultured hippocampal neurons, an effect which is the opposite of that induced by anandamide.. PGD2-EA also induces apoptosis in colorectal carcinoma cell lines.

Prostaglandin D2 serinol amide serves as a mild inhibitor against the hydrolysis of [3H]2-oleoylglycerol [1].

15-deoxy-Δ12,14-Prostaglandin D2 (15-deoxy-Δ12,14-PGD2) is a PGD2 metabolite functioning as an agonist for the PGD2 receptor 2 (DP2), with a binding affinity (Ki) of 50 nM for the mouse DP2 receptor expressed in HEK293 cell membranes. It activates eosinophils with an EC50 of 8 nM and enhances the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), initiating PPARγ-mediated transcription at 5 µM concentration. Furthermore, it exhibits cytotoxicity towards L1210 murine leukemia cells with an IC50 of 0.3 µg/ml and displays weaker inhibition of ADP-induced platelet aggregation than PGD2, with an IC50 of 320 ng/ml.

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].

Prostaglandin D2 (PGD2) is a primary enzymatic prostaglandin derived from PGH2 and is abundantly produced in the cerebrospinal fluid (CSF) by the lipocalin-type PGD synthase, and peripherally by myeloid cells such as mast cells and basophils via a hematopoietic-type PGD synthase. PGD2 is chemically unstable and presents challenges for use and analysis due to its brief in vivo half-life. Δ12-PGD2, an initial decomposition product of PGD2, acts as an intermediate in the pathway to Δ12-PGJ2, a cyclopentenone prostaglandin known for its antimitotic and carcinogenic properties. The metabolism of Δ12-PGD2 involves the addition of thiol nucleophiles, a common pathway for many cyclopentenone prostaglandins.

Prostaglandin D2 (PGD2) is one of the five principal prostaglandins enzymatically derived from PGH2. It is abundantly generated in the cerebrospinal fluid (CSF) by lipocalin-type PGD synthase and in peripheral regions by myeloid cells, such as mast cells and basophils, via leukocyte-type PGD synthase. The compound 1,25-trans-PGD2 is an isomer of PGD2, characterized by the alteration of the double bond between carbons 5 and 6 from cis(Z) to trans(E). This trans isomer, found as a 2-5% impurity in most commercial PGD2 bulk drug preparations, is primarily synthesized as an analytical standard to identify and quantify this impurity. Based on existing studies of trans isomers of F-type prostaglandins, 5-trans-PGD2 likely exhibits biological activity comparable to its cis isomer, although no specific published reports confirm this for 5-trans-PGD2.

13,14-Dihydro-15-keto prostaglandin D2 (DK-PGD2), a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway, is a selective agonist for the DP2 receptor and can inhibit ion flux in canine colonic mucosa preparation [1].

16,16-dimethyl PGD2 is a metabolically stable synthetic analog of PGD2. It enhances ADP-induced human platelet aggregation and increases systemic blood pressure in rats.

Prostaglandin D2-1-glyceryl ester (PGD2-G; PGD2 2-glyceryl ester) is a chemical compound known for its significance in various biological processes. This compound, commonly referred to by its abbreviations PGD2-G or PGD2 2-glyceryl ester, plays a crucial role in the mediation of physiological functions.

Prostaglandin D2 (Standard) is a reference standard for research and analysis in studies involving Prostaglandin D2. Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals,and is a potent endogenous sleep promoting substances.

Nedocromil (FPL 59002) inhibits the action or formation of multiple mediators. Which including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).

AM211 (AM211 free acid) is a potent and orally bioavailable antagonist of prostaglandin D2 (PGD2) receptor type 2 (DP2)

11-Keto Fluprostenol, a potent analog of prostaglandin F2α (PGF2α), primarily interacts with the FP receptor. It is a structurally modified derivative of prostaglandin D2 (PGD2) designed to enhance its potency and extend its half-life. The compound is produced by oxidizing fluprostenol at the C-11 position, which results in 11-keto fluprostenol. This modification allows 11-keto Fluprostenol to exhibit moderate affinity for the CRTH2/DP2 receptor, though it shows negligible activity at the DP1 receptor, distinguishing its action from that of PGD2.

PROTAC(H-PGDS)-7 is a selective and potent small molecule hematopoietic prostaglandin D synthase (H-PGDS) PROTAC degradation agent that exhibits degradation activity in KU812 cells with a DC50 of 17.3 pM. It effectively inhibits prostaglandin D2 (PGD2) and is a candidate compound for the treatment of DMD and other H-PGDS-related diseases.

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.

CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.

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).

L 888607 Racemate is a selective antagonist of the prostaglandin D2 receptor subtype 1 (DP1) with Ki values of 132 nM and 17 nM for DP1 and the thromboxane A2 receptor (TP), respectively.

AT56, a specific inhibitor of prostaglandin D2 synthase enzymatic activity, blunted adipogenic aldosterone effects.