GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain[1].
OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM.IC50 Value: 13 nM( Ki for hrCRTH2); 3 nM( Ki for Rat rCRTH2);13 nM(Ki for human native CRTH2)Target: D prostanoid receptor 2CRTH2 (chemoattractant receptor expressed on T-helper (Th) type 2 cells) is a G-protein-coupled receptor expressed by Th2 lymphocytes and eosinophils that mediates prostaglandin (PG)D(2)-driven chemotaxis[1]. CRTH2 mediates activation of Th2 cells, eosinophils and basophils in response to prostaglandin D(2). The CRTH2 antagonist OC000459 has been demonstrated to reduce airway inflammation and improve lung function in moderate persistent asthma[2].in vitro: OC000459 is an indole-acetic acid derivative that potently displaces [3H]PGD2from human recombinant DP2 (Ki = 0.013 μM), rat recombinant DP2 (Ki = 0.003 μM), and human native DP2 (Th2 cell membranes; Ki = 0.004 μM) but does not interfere with the ligand binding properties or functional activities of other prostanoid receptors (prostaglandin E1-4 receptors, D prostanoid receptor 1, thromboxane receptor, prostacyclin receptor, and prostaglandin F receptor). OC000459 inhibited chemotaxis (IC50 = 0.028 μM) of human Th2 lymphocytes and cytokine production (IC50 = 0.019 μM) by human Th2 lymphocytes. OC000459 competitively antagonized eosinophil shape change responses induced by PGD2 in both isolated human leukocytes (pKB = 7.9) and human whole blood (pKB = 7.5) but did not inhibit responses to eotaxin, 5-oxo-eicosatetraenoic acid, or complement component C5a. OC000459 also inhibited the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells. OC000459 had no significant inhibitory activity on a battery of 69 receptors and 19 enzymes including cyclooxygenase 1 (COX1) and COX2[3] .in vivo: OC000459 was found to be orally bioavailable in rats and effective in inhibiting blood eosinophilia induced by 13,14-dihydro-15-keto-PGD2 (DK-PGD2) in this species (ED50 = 0.04 mg/kg p.o.) and airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED50 = 0.01 mg/kg p.o.) [3].Clinical trial: N/A.
ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer[1].
EP2 receptor antagonist-2 (CID891729) is an antagonist of EP2 receptor. EP2 receptor antagonist-2 inhibits the EP2 receptor activation induced by PGE2. EP2 receptor antagonist-2 also suppresses lactate dehydrogenase (LDH) release induced by N-methyl-D-aspartate (NMDA)[1].
KW-8232, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2[1].
Ro 22-9194 inhibits aggregation and thromboxane Az (TXA2) synthetase activity in rabbit and human platelets. Ro 22-9194 has a potent inhibitory action against various types of model arrhythmias. Ro 22-9194 has non-cholinergic cardiac depressant properties with its vasodilating action[1][2].
Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
AL-3138 (11-Deoxy-16-fluoro PGF2α) is a prostaglandin F2 alpha (PGF2alpha) analogue that antagonises FP prostaglandin receptor-mediated inositol phosphate production[1].
Prostaglandin E1-d4 (Alprostadil-d4) is the deuterium labeled Prostaglandin E1. Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases[1][2][3].
MK-8318 is potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
Darbufelone 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).
BAY-1316957 is a highly potent and selective EP4 receptor antagonist with an IC50 of 15.3 nM. Good oral bioavailability[1].
ONO 1301 (ONO-AP 500-02), a prostaglandin (PG) I2 mimetic, is an orally active, long-acting prostacyclin agonist with thromboxane-synthase inhibitory activity. ONO 1301 promotes production of hepatocyte growth factor (HGF) from various cell types and ameliorates ischemia-induced left ventricle dysfunction in the mouse, rat and pig[1][2][3].
ICI 192605 is a potent TXA2R (thromboxane A2 receptor) antagonist as cell signaling prostaglandin. ICI 192605 blocks contraction of isolated guinea pig trachea induced by U-46619[1].
KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.
NCX 470 is a second-generation nitric oxide (NO)-donating prostaglandin analogue. NCX 470 effectively lowers intraocular pressure (IOP) in animal models of ocular hypertension and glaucoma by activating bimatoprost-mediated uveoscleral outflow and NO mediated conventional outflow. NCX 470 can be used for the research of cular hypertension and glaucoma[1][2].
Prostaglandin J2 (PGJ2), an endogenous metabolite of Prostaglandin D2 (PGD2; HY-101988), is a potent PGD2 receptor (DP) agonist with Kis of 0.9 nM and 6.6 nM for hDP and hCRTH2, respectively. Prostaglandin J2 stimulates intracellular cyclic AMP production with an EC50 value of 1.2 nM. Prostaglandin J2 induces oxidative stress and neuronal apoptosis. Prostaglandin J2 induces the accumulation/aggregation of ubiquitinated (Ub) proteins. Prostaglandin J2 is highly neurotoxic and potentially contributes to many neurodegenerative conditions, including Alzheimer's (AD) and Parkinson's diseases (PD)[1][2][3][4].
Tafluprost acid (AFP-172), an active metabolic form of Tafluprost, is a selective prostanoid FP receptor agonist. Tafluprost acid shows a high affinity for human prostanoid FP receptor with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC50=67 nM) than for the prostanoid FP receptor. Tafluprost acid can be used in the research of glaucoma[1][2][3].
CJ-42794 is a selective prostaglandin E receptor subtype 4(EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3).IC50 value: 8.5 (pKi ) [1]Target: EP4in vitro: CJ-042794 competitively inhibits PGE2-evoked elevations of intracellular cAMP levels in HEK293 cells overexpressing human EP4receptor with a mean pA2 value of 8.6. PGE2 inhibits the lipopolysaccharide (LPS)-induced production of tumor necrosis factor α (TNFα) in human whole blood (HWB); CJ-042794 reverses the inhibitory effects of PGE2 on LPS-induced TNFα production in a concentration-dependent manner. [1]in vivo: CJ-42794 significantly delays the ulcer healing in rats and mice. The expression of VEGF in primary rat gastric fibroblasts was increased by PGE2 or AE1-329 (EP4 agonist), and these responses were both attenuated by coadministration of CJ-42794.[2]
15-Keto latanoprost is a metabolite of Latanoprost, which is an ocular hypotensive agent[1].
Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor[1][2].
PF-04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist with IC50 of 16 nM, displays >2000-fold functional selectivity for the human EP2 receptor over antagonist activity against the human EP1, EP3, EP4, DP1 and CRTH2 receptors.IC50 value: 16 nMTarget: EP2in vitro: PF-04418948 inhibits prostaglandin E2 (PGE2)-induced increase in cAMP in cells expressing EP2 receptors with a functional KB value of 1.8 nM. In human myometrium, PF-04418948 produced a parallel, rightward shift of the butaprost-induced inhibition of the contractions induced by electrical field stimulation with an apparent KB of 5.4 nM. [1]in vivo: In dog bronchiole and mouse trachea, PF-04418948 produced parallel rightward shifts of the PGE2-induced relaxation curve with a KB of 2.5 nM and an apparent KB of 1.3 nM respectively. Reversal of the PGE2-induced relaxation in the mouse trachea by PF-04418948 produced an IC50 value of 2.7 nM. Given orally, PF-04418948 attenuated the butaprost-induced cutaneous blood flow response in rats. [1] PF-04418948 competitively inhibits relaxations of murine and guinea pig trachea induced by ONO-AE1-259 and PGE2 respectively.[2]
Laropiprant is a potent, selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.
TCS 2510 is a selective EP4 agonist. TCS 2510 can be used for the research of metabolic diseases[1].
LCB-2853 is an antagonist of thromboxane A2 (TXA2) receptor, with antiplatelet and antithrombotic activities.
Benorylate (Benoral) is the esterification product of paracetamol and acetylsalicylic acid. It has anti-inflammatory, analgesic and antipyretic properties. Benorylate could also inhibit prostaglandin (PG) synthesis.
Pectolinarin, isolated from Cirsium chanroenicum, possesses anti-inflammatory activity[1]. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin suppresses cell proliferation and inflammatory response and induces apoptosis via inactivation of the PI3K/Akt pathway[2].
CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model[1][2][3].
Selexipag-d6 is deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.