KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors[1].
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.
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
Prostaglandin E1 (PGE1) is a potent vasodilator and activates the prostaglandin E1 (EP) receptor.
(+)-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].
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.
HHS-0701, a sulfur-triazole exchange (SuTEx) ligand, is a potent tyrosine-reactive prostaglandin reductase 2 (PTGR2) inhibitor. HHS-0701 blocks PTGR2 metabolism of the lipid substrate 15-Keto-PGE2[1].
Dinoprost(Prostaglandin F2α) tromethamine salt is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
Bimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension.Target: Prostaglandin ReceptorBimatoprost is a prostaglandin analog/prodrug used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. It reduces intraocular pressure (IOP) by increasing the outflow of aqueous fluid from the eyes. In December 2008, the indication to lengthen eyelashes was approved by the U.S. Food and Drug Administration (FDA); the cosmetic formulation of bimatoprost is sold as Latisse. In 2008-2011, at least three case series suggested that bimatoprost has the ability to reduce adipose (fat) tissue.Bimatoprost activates prostamide alpha F2 receptors found in the hair follicle to stimulate its growth rate. Research led by Professor Randall and the University of Bradford found that it may also offer a treatment for scalp hair regrowth in trials conducted on samples taken from men undergoing hair transplants. According to Allergan's package labeling, users of its Latisse cosmetic product didn't develop darker irises in clinical studies; however, "patients should be advised about the potential for increased brown iris pigmentation which is likely to be permanent."
Treprostinil palmitil (TP) is the prodrug of DP1 and EP2 agonist, Treprostinil (UT-15), whose EC50 values were 0.6 and 6.2 nM, respectively. Treprostinil palmitil is a pure prodrug and possesses no inherent binding to G-protein coupled receptors including prostanoid receptors[1][2].
11-Deoxy Prostaglandin E2 is a selective agonist of EP4 with an EC50 of 0.66 nM. 11-Deoxy Prostaglandin E2 is an analog of prostaglandin E2. 11-Deoxy Prostaglandin E2 can be used in study bone healing, heart failure, and other receptor associated conditions[1][2].
U66858 is a potent inhibitor of LTB4 production in human whole blood. U66858 also exhibits significant inhibition of lipoxygenase and TXB2 release.
Agnuside is a compound isolated from Vitex negundo, down-regulates pro-inflammatory mediators PGE2 and LTB4, and reduces the expression of cytokines, with anti-arthritic activity[1].
AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour[1].
BGC-20-1531 (PGN 1531) free base is a potent and selective prostanoid EP4 receptor antagonist, with a pKb of 7.6. BGC-20-1531 free base has the potential for the research of migraine headache[1].
Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.
BAY 73-1449 is a selective antagonist of prostacyclin IP receptor, with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure[1].
Latanoprost is an agonist for the FP prostanoid receptor, and lowers intraocular-pressure (IOP).
AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors.IC50 Value: ~3 nM (EC50 for calcium mobilization by PGE2) [1]Target: EP/DP receptorin vitro: AH6809also antagonized the aggregatory effect of U-46619 in whole blood (pA2 = 4.45). However, concentrations of AH6809 up to 300 microM were without effect upon either ADP- or platelet activating factor (Paf)-induced aggregation (pA2 less than 3.5) [2]. Preincubation of control cells in 10(-4) M concentrations of AH6809 inhibited PGE2-induced activation of AC by greater than 80% without significant (P greater than .05) inhibition of basal activity by the antagonist [3].in vivo: Exposure to a selective COX-2 inhibitor (SC58125) or an EP1/EP2 antagonist (AH6809), but not an EP4 antagonist (AH23848B), significantly reduced cell proliferation of esophageal explants in 24 hour-organ culture experiments [4]. Oral administration of the EP1 receptor antagonist, AH6809 (10 mg/kg/day, for 4 days), significantly reduced the systolic blood pressure in db/db, but not in control mice [5].
PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca2+-dependent large-conductance K+-channel in human myometrial cells[1][2].
CRTh2 antagonist 1 is a CRTh2 antagonist with an IC50 of 89 nM。
MF266-3 is a potent, selective prostaglandin E receptor subtype 3 (EP3) antagonist with Ki of 0.8 nM; displayes a relatively good selectivity over other prostanoid receptors.
TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors. IC50 value: 7.5 μMTarget: serotonin 5-HT2B receptorin vitro: TG6-10-1, an analog of TG4-155 (a prostaglandin receptor EP2 antagonist, with a relatively short plasma half-life (0.6 h) and low brain:plasma ratio (0.3) after systemic administration in mice), which has a superior pharmacokinetic profile making it suitable for more extensive testing. TG6-10-1 had negligible effect on a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s > 10 μM), except that TG6-10-1 weakly inhibited the serotonin 5-hydroxytryptamine 2B (5-HT2B) receptor with IC50 = 7.5 μM. At a high concentration (10 μM), TG6-10-1 had little or no effect on the enzymatic activity of COX-1 (7% inhibition) and COX-2 (14% inhibition), and inhibited the leukotriene B4 (LTB4) receptor BLT1 by 1% .EP2 receptor activation by PGE2 stimulates adenylate cyclase to elevate cytoplasmic cAMP level. TG6-10-1 has a competitive mechanism of antagonism of the EP2 receptor with an equilibrium dissociation constant for the antagonist-receptor complex (KB) of 17.8 nM.in vivo: TG6-10-1 displayed a plasma half-life of 1.6 h and a brain:plasma ratio of 1.6 after systemic administration (5 mg/kg, i.p.) in mice. A significant increase in survival was observed in post-SE mice that received TG6-10-1 compared with those in the vehicle group. Administration of TG6-10-1 improved 1-wk survival from 60 to 90% after SE.
L 888607 is a potent, and selective CRTH2 (also known as DP2) agonist with a Ki of 0.8±0.4 nM.
GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4.
CAY10590 (GK115) is an inhibitor of secreted phospholipase A2 (sPLA2) and can be used for the research of chronic inflammatory kidney diseases[1].
CP-544326 is a potent and selective prostaglandin E2 receptor agonist with an EC50 of 2.8 nM.
SQ 29548, a high affinity radioligand, is a selective thromboxane-prostanoid (TP) receptor antagonist[1][2].
Epibetulinic acid, isolated from the root bark of Maytenus cuzcoina and the leaves of Maytenus chiapensis, exhibits potent inhibitory effects on NO and prostaglandin E2 (PGE2) production in mouse macrophages (RAW 264.7) stimulated with bacterial endotoxin with IC50s of 0.7 and 0.6 μM, respectively. Anti-inflammatory activity[1].