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[1].trans-isoferulic acid suppresses NO and PGE2 production through the induction of Nrf2-dependent heme oxygenase-1 (HO-1)[2].
Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor[1]. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes[2].
Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.
Amtolmetin guacil is an effective nonsteroidal anti-Inflammatory agent with pain-relieving effects. Amtolmetin guacil inhibits prostaglandin synthesis and cyclooxygenase (COX). Amtolmetin guacil can stimulate capsaicin receptors present on the gastrointestinal wall and also releases gastroprotective nitric oxide (NO). Amtolmetin guacil can be used to research knee osteoarthritis[1][2].
Seratrodast(AA 2414) is a potent and selective thromboxane A2 receptor (TP) antagonist.Target: Thromboxane A2 ReceptorSeratrodast, also known as AA-2414, is a potent and selective antagonist of the TXA2R (thromboxane A2 receptor). AA-2414 reduced the induction of pulmonary inflation caused by LTD4 aerosol inhalation. AA-2414 competitively inhibited the contractile response to U-46619 in guinea pig tracheal and parenchymal strips and dog saphenous vein strips with pA2 values of 7.69, 8.29 and 6.79, respectively. AA-2414, a quinone derivative, is a novel, potent and orally active antagonist of a variety of spasmogenic prostanoids [1]. AA-2414 inhibited peroxide-induced vasoconstriction in the human placenta, as well as peroxide- induced increases in the placental secretion rates of lipid peroxides and thromboxane, but only partially inhibited peroxide-induced increases in the placental secretion rate of prostacyclin [2].
MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.
Aganepag isopropyl (AGN-210961) is an EP2 agonist[1][2].
MK-2894 is a highly potent and selective second generation EP4 antagonist.IC50 value:Target: EP4MK-2894 exhibits favorable pharmacokinetic profile in a number of preclinical species and potent anti-inflammatory activity in several animal models of pain/inflammation. MK-2894 also shows favorable GI tolerability profile in rats when compared to traditional NSAID indomethacin.
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.
Taprostene (CG-4203) is a synthetic, chemically stable analogue of Prostacyclin (PGI2). Taprostene exhibits endothelium and myocardial protecting actions after acute myocardial ischemia and reperfusion in cats. Taprostene enhances cytoprotective actions, while minimizing unwanted hemodynamic effects[1].
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].
Etersalate inhibits platelet function and decreases thromboxane A2 (TXA2) levels.
Ethamsylate is a haemostatic drug, also inhibits biosynthesis and action of those prostaglandins.
U-46619 (9,11-Methanoepoxy PGH2) is a stable analogue of thromboxane A2 (TXA2) and acts as a potent TXA2 agonist[1].
TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM[1][2]. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1[1]. TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor[2].
Laropiprant sodium is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively[1][2][3].
ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist.
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor[1].
LAS191859 is an orally active, potent and selective CRTh2 antagonist with an IC50 of 9.58 nM against human CRTh2. LAS191859 can be used for the research of chronic asthma[1].
QCC374 is a selective agonist of IP[1].
Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2).Target: prostaglandin receptorin vitro: Grapiprant is a novel pharmacologically active ingredient, acts as a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). [1]in vivo: Grapiprant is currently under development for use in humans and dogs for the control of pain and inflammation associated with osteoarthritis. [1] Results suggested the safety of long-term oral administration of grapiprant to dogs. Efficacy of grapiprant in the treatment of dogs with osteoarthritis needs to be evaluated in other studies. [2]
Ginsenoside Ro exhibits a Ca2+-antagonistic antiplatelet effect with an IC50 of 155 μM. Ginsenoside Ro reduces the production of TXA2 more than it reduces the activities of COX-1 and TXAS.
Prostaglandin D3 (PGD3) is a prostaglandin that acts as an inhibitor of platelet aggregation and a modulator of autonomic neurotransmission in humans[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].
p-Hydroxycinnamic acid, a common dietary phenol, could inhibit platelet activity, with IC50s of 371 μM, 126 μM for thromboxane B2 production and lipopolysaccharide-induced prostaglandin E2 generation, respectively.
AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.
AH23848 hemicalcium salt is a potent, specific and orally active thromboxane receptor blocker. AH23848 hemicalcium salt inhibits platelet deposition[1].
Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.
EP3 antagonist 3 (compound 2) is an orally active, potent and selective EP3 antagonist, with a pKi of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research[1].
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM)[1].