MF-766 (MF766) is a highly potent and selective EP(4) antagonist with binding Ki of 0.23 nM, displays no significant affinity (>7000-fold selectivity) against other PG receptors (IC50>1500 nM); behaved as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay; exhibits blockade of inhibition of TNFa-induced IP10 release by the specific EP4 agonist L-000902688 (IC50=9.5 nM); demonstrates potency and efficacy of in the rat AIA model measuring inhibition of paw swelling.
Dazoxiben is a potent and orally active thromboxane (TX) synthase inhibitor[1].
FR181157, an orally active PGI2 agonist activity with especially good pharmacokinetic properties[1].
Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals high affinity to ER-α and PGE2 receptor (EP2 subtype) with Ki values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities[1].
BMY 45778 is a non-prostanoid prostacyclin mimetic. BMY 45778 inhibits human (IC50 = 35 nM), rabbit (IC50: 136 nM) and rat (IC50 : 1.3 μM) platelet aggregation. BMY 45778 also activates adenylyl cyclase. BMY 45778 is a partial agonist at the prostacyclin receptor[1].
Darbufelone mesylate is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
BGC20-1531 (PGN-1531, AP 1531) is a potent, selective prostanoid EP receptor EP antagonist, exhibits high affinity at recombinant human EP4 receptors expressed in cell lines (pKB=7.6) and native EP4 receptors in human cerebral and meningeal artery (pKB=7.6-7.8); shows no appreciable affinity at a wide range of other receptors (including other prostanoid receptors), channels, transporters and enzymes (pKi < 5); competitively antagonizes PGE(2)-induced vasodilatation of human middle cerebral (pK(B) 7.8) and meningeal (pK(B) 7.6) arteries in vitro, and PGE(2)-induced increase in canine carotid blood flow in vivo. Migraine Phase 2 Discontinued
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].
Prostaglandin E1 (PGE1) is a potent vasodilator and activates the prostaglandin E1 (EP) receptor.
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].
Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers[1]. Misoprostol is an oral agent used to induce labor[2].
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].
GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC50 of 7.9.
Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
TP-16 is a novel and selective EP4 antagonist with an IC50 of 2.1 nM.
15-keto-Prostaglandin E2 is an endogenous metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to its Cys259 residue. 15-keto-Prostaglandin E2 can bind and stabilize EP2 and EP4 receptor. 15-keto-Prostaglandin E2 inhibits breast cancer cell growth and progression. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth[1][2][3].
MRE-269-d6 is deuterium labeled MRE-269. MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
(+)-Cloprostenol is a prostaglandin F2α (PGF2α) analogue, and shows selective agonistic activity at the prostaglandin receptor.
Thromboxane B1 (TXB1) is one of thromboxane B (TXB) family members. Thromboxane is a member of the family of lipids known as eicosanoids. Thromboxane is named for its role in blood clot formation (thrombosis)[1].
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].
DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier[1][2].
CAY10580 is a potent and selective prostaglandin EP4 receptor agonist (Ki=35 nM)[1].
Cloprostenol isopropyl ester, a prostaglandin F2α analogs, is the intermediate of (+)-Cloprostenol (HY-107381). Cloprostenol isopropyl ester is a FP receptor agonist with a Ki value of 28 nM[1][2].
AZ-1355 is an effctive lipid-lowering compound, which also inhibits platelet aggregation in vivo and elevates the prostaglandin I2/thromboxane A2 ratio in vitro.
MRE-269-d7 is deuterium labeled MRE-269 (HY-79593). MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist[1][2].