Prostaglandin E1-d9 is deuterium labeled Prostaglandin E1.Prostaglandin E1 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 inh
Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity[1]. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension[2].
Sulprostone (SHB 286), a prostaglandin E2 (PGE2) analogue, is a potent and selective EP3 receptor agonist. Sulprostone has potential antiulcer and nonsteroidal abortifacient effects used for the research of pregnancy termination and hemorrhages during delivery[1][2][3].
AGN 210676 is a selective prostaglandin EP2 agonist extracted from patent US20070203222A1, Compound example 23, has an EC50 of 5 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.
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].
BAY-6672 hydrochloride is a potent and selective human Prostaglandin F (FP) receptor antagonist with an IC50 value of 11 nM.
CGS 15435, a potent thromboxane (TxA2) synthetase inhibitor with an IC50 of 1 nM, has a selectivity for Tx synthetase 100000-fold greater than that for cyclooxygenase, PGI2 synthetase and lipoxygenase enzymes.
AZD1981 is a potent and selective CRTh2 antagonist; displaces radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4).IC50 value:Target: GPR44 antagonistin vitro: AZD1981 produced a concentration-dependent displacement of the [3H]PGD2-specific binding with a mean pIC50 of 8.4 ± 0.1 (n = 25, geometric mean IC50 of 4 nM). AZD1981 had no significant affinity towards recombinant human DP1 receptors with only a mean 27% (range 14–50%; n = 4) displacement of [3H]PGD2-specific binding observed at the highest concentration tested (10 μM). Compared with the binding potency for DP2, AZD1981 showed 10-fold selectivity over rat aldose reductase and 1700-fold selectivity over rat steroid 5α-reductase.In eosinophils, a single concentration of 1 μM, AZD1981 caused a large (20-fold) rightward parallel shift in the 15R-methyl PGD2 E/[A] curve with no evidence of a decrease in the maximal response. The effect of AZD1981 was therefore investigated using a single sub-maximal concentration of agonist (1 μM). AZD1981 produced a concentration-dependent inhibition of eosinophil migration with a pIC50 value of 7.6 ± 0.1 (n = 4) [1].in vivo: Using the previously described guinea pig hind limb model , 10 nM AZD1981 significantly inhibited DK-PGD2-induced eosinophil mobilization by approximately 50%, and the response was completely inhibited with 100 nM AZD1981 [1]. in vivo: AZD1981 exhibited good cross-species binding activity against mouse, rat, guinea pig, rabbit and dog DP2 . Evaluation in mouse, rat or rabbit cell systems was not possible as they did not respond to DP2 agonists. Agonist responses were seen in guinea pig and dog, and AZD1981 blocked DP2 -mediated eosinophil shape change. Such responses were more robust in the guinea pig, where AZD1981 also blocked DP2 -dependent eosinophil emigration from bone marrow [1]. There was no beneficial clinical effect of AZD1981, at a dose of 1000 mg twice daily for 4 weeks, in patients with moderate to severe COPD. AZD1981 was well tolerated and no safety concerns were identified [3].
Aganepag is a potent Prostanoid EP2 receptor agonist, with an EC50 of 0.19 nM, and shows no activity at EP4 receptor. Aganepag can be used in the research of wound healing, scar reduction, scar prevention and wrinkle treatment and prevention.
EP4 receptor antagonist 4 is an EP4 receptor agonist with the human pEC50 value of 6.3[1].
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].
Furprofen is an non-steroidal anti-inflammatory drug (NSAID) with analgesic properties[1]. Furprofen acts via the inhibition of prostaglandin (PGE) synthesis. Furprofen can be treated orally for the relief of pain[2][3].
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury[1][2].
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.
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].
GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4.
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]
MF498 is a novel and selective E prostanoid receptor 4 (EP4 receptor) antagonist, displayed strong binding affinity for the EP4 receptor with Ki of 0.7 nM.Ki value: 0.7 nMTarget: EP4 receptorin vitro: MF498 also displays a relatively good selectivity over other prostanoid receptors, does not compromise the mucosal integrity in the gastrointestinal tract.MF498 inhibits PGE2-stimulated cAMP accumulation in a dose-dependent manner with IC50 values of 1.7 and 17 nM in the absence and presence of 10% serum, respectively. in vivo: MF498 relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis. MF498 on inflammation in adjuvant-induced arthritis (AIA), a rat model for rheumatoid arthritis (RA), and joint pain in a guinea pig model of iodoacetate-induced osteoarthritis (OA).
CAY10590 (GK115) is an inhibitor of secreted phospholipase A2 (sPLA2) and can be used for the research of chronic inflammatory kidney diseases[1].
Terutroban is a thromboxane-prostaglandin receptor antagonist.
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.
Iloprost-d4 (Ciloprost-d4) is the deuterium labeled Iloprost. Iloprost (ZK 36374) is a synthetic analogue of prostacyclin PGI2[1][2].
TCS 2510 is a selective EP4 agonist. TCS 2510 can be used for the research of metabolic diseases[1].
Nocloprost, a prostaglandin E2 (PGE2) analog, is an orally active EP1- and EP3-receptor agonist. Nocloprost inhibits evoked [3H]ACh release. Nocloprost has gastroprotective and ulcer-healing properties. Nocloprost accelerates the healing of chronic gastric ulcerations and enhances mucosal growth in rats[1][2].
LCB-2853 is an antagonist of thromboxane A2 (TXA2) receptor, with antiplatelet and antithrombotic activities.
Pexopiprant is an oral antagonist of the prostaglandin D2 receptor 2 (DP2),Ki ＜ 100nM. Pexopiprant can be used in studies of asthma[1].
CP-544326 is a potent and selective prostaglandin E2 receptor agonist with an EC50 of 2.8 nM.