15-keto-Prostaglandin F2α (15-keto-PGF2α) is a metabolite of Prostaglandin F2α. Prostaglandin F2α. Prostaglandin F2α is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist and plays a key role in the onset and progression of labour[1].
CI-949 is an allergic mediator release inhibitor, which inhibits histamine, leukotriene C4/D4 (LTC4/LTD4), and thromboxane B2 (TXB2) release with IC50s of 11.4 μM, 0.5 μM and 0.1 μM, respectively.
EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects[1].
Picotamide is a combined inhibitor of thromboxane A2 (TxA2) synthase and receptor. Picotamide has antiplatelet activity. Picotamide promotes the reduction of microalbuminuria and the inhibition of growth of carotid plaques in diabetes. Picotamide can be used for researching acute or chronic cardiovascular diseases[1].
Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2.IC50 value: 6.0 nMTarget: PGD2in vitro: Setipiprant is an orally available, selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T helper [Th]-2 cells) antagonist. CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced by the mast cells and is a key mediator in various inflammatory diseases, including allergy and asthma. Binding of PGD2 to CRTH2, which are expressed on the surface of blood-borne cells, induces chemotaxis of Th2 cells, basophils, and eosinophils, and stimulates cytokine release from these cells. Thus, antagonism of CRTH2 receptors is considered to be a promising therapeutic target for various allergic diseases and asthma.
I-SAP is a radioiodinated TXA2/PGH2 receptor antagonist. The bind between I-SAP and the receptors, is inhibited by the histidine modifying reagent diethyl-pyrocarbonate (DEPC)[1][2].
ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist.
QCC374 is a selective agonist of IP[1].
Treprostinil (UT-15C) diethanolamine is a potent EP2, DP1 and IP agonist with Ki values of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1, IP, EP1, EP4, EP3 and FP, respectively. Treprostinil (UT-15C) diethanolamine increases upregulation of cAMP toward maintaining homeostasis within the vasculature. Treprostinil (UT-15C) diethanolamine can result in vasodilatation of human pulmonary arteries[1][2][3].
Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.
Satigrel (E5510) is a potent inhibitor of platelet aggregation. Satigrel inhibits collagen- and arachidonic acid-induced platelet aggregation through preventing thromboxane A2 synthesis by selective inhibition of the target enzyme, PGHS1, which exists in platelets. Satigrel inhibits PGHS1 (IC50: 0.081 μM) and PGHS2 (IC50: 5.9 μM). Satigrel is against Type III PDE, Type V and Type II (IC50: 15.7 μM, 39.8 μM and 62.4 μM, respectively)[1].
L 640035 is athromboxaneantagonist[1].
Ridogrel (R 68070) is an orally active combined thromboxane A2 synthetase inhibitor and thromboxane A2/prostaglandin endoperoxide receptor blocker. Ridogrel is potent antiplatelet agent. Anti-inflammatory activities[1][2][3].
16,16-Dimethyl prostaglandin E2 (16,16-dimethyl PGE2) is an orally active vertebrate Hematopoietic stem cells (HSCs) homeostasis critical regulator. 16,16-Dimethyl prostaglandin E2 can act through EP2/EP4 and has an interaction with the Wnt pathway[1][2].
Selexipag-d8 (NS-304-d8) is the deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor)[1][2].
EP4-IN-1 is a potent prostanoid EP4 receptor inhibitor. EP4-IN-1 is extracted from patent WO2023025270 (example 1), and exhibits prospect in tumor immunity and anti-inflammatory analgesia research[1].
Vorbipiprant (CR6086) is an EP4 receptor antagonist, serving as a targeted immunomodulator. Thus, Vorbipiprant is also a potential immune checkpoint inhibitor, to turn cold tumors into hot tumors. Vorbipiprant also antagonizes PGE2-stimulated cAMP production (IC50=22 nM). Vorbipiprant exhibit striking DMARD effects in rodents, and anti-inflammatory activity to inhibt immune-mediated inflammatory diseases[1][2].
trans-Isoferulic acid-d3 is the deuterium labeled trans-Isoferulic acid[1]. trans-Isoferulic acid (trans-3-Hydroxy-4-methoxycinnamic acid) is an aromatic acid isolated from the roots of Clematis florida var. plena. trans-Isoferulic acid exhibits anti-inflammatory activity[2].trans-isoferulic acid suppresses NO and PGE2 production through the induction of Nrf2-dependent heme oxygenase-1 (HO-1)[3].
Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
Beraprost sodium, a prostacyclin analog, is a stable and orally active prodrug of PGI2. Beraprost sodium is a potent vasodilator, has the potential for pulmonary arterial hypertension treatment through expanding renal vessels, improving microcirculation[1].
SC-51089 is a selective antagonist of EP1 receptor with analgesic activity in vivo[1].
1a,1b-Dihomo prostaglandin E1 (1a,1b-Dihomo PGE1) is a class of prostaglandin compound[1].
Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils[1].
Rebamipide is an inducer of endogenous prostaglandin and a oxygen-derived free radical scavenger.Target: OthersRebamipide is the first anti-gastric ulcer and antigastritis drug that not only increases endogenous prostaglandin in gastric mucosa but also scavenges oxygen-derived free radicals and inhibits their production. The inhibitory effect of rebamipide on lipid peroxidation induced by a free radical initiator was also demonstrated by the in vitro system using rat gastric mucosal homogenates. These data indicate that rebamipide offers a potential for protection against reactive oxygen- and activated neutrophil-associated gastric mucosal injury by scavenging hydroxyl radical and inhibiting neutrophil activation or lipid peroxidation [1]. Rebamipide can contribute to the management of patients who are taking NSAIDs or are infected with H. pylori. Rebamipide may enhance eradication of H. pylori-infection using standard eradication therapy [2]. Rebamipide is beneficial for obtaining a better quality of ulcer healing and reduction of future ulcer relapse [3].
SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity[1][2][3].
GSK-269984B is a potent EP1 antagonist. GSK-269984B has the potential for inflammatory pain research[1].
TP-16 is a novel and selective EP4 antagonist with an IC50 of 2.1 nM.
MRE-269-d6 is deuterium labeled MRE-269. MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
Omidenepag,a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC50 of 1.1 nM. Omidenepag shows binding affinities (IC50) 10 nM for h-EP2[1].
LG 82-4-01 is a thromboxane (TX) synthetase specific inhibitor, with an IC50 of 1.3 μM[1].