Cloprostenol sodium salt (ICI 80996 sodium salt) is a potent synthetic prostaglandin analogue, acts as a PGF2α receptor agonist[2] and is a luteolytic agent[1].
MK-447 is a free radical scavenger, also a nonsteroidal antiinflammatory agent, and enhances the formation of the endoperoxide, PGH2, and other prostaglandins.
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].
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).
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].
Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
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].
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].
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].
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].
BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively[1]. BI-671800 has potential for the treatment of poorly controlled asthma[2].
GW627368(GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor(Ki= 100 nM) with additional human TP receptor affinity(Ki= 150 nM).IC50 value: Target: EP4 antagonistin vitro: At recombinant human prostanoid EP4 receptors expressed in HEK293 cells, GW627368X produced parallel rightward shifts of PGE2 concentration-effect (E/[A]) curves resulting in an affinity (pKb) estimate of 7.9 +/- 0.4. GW627368X appears to bind to human prostanoid TP receptors but not the TP receptors of other species. In human washed platelets, GW627368X (10 microM) produced 100% inhibition of U-46619 (EC100)-induced aggregation (approximate pA2 approximately 7.0) [1]. in vivo: Oral administration of GW627368X showed significant tumor regression characterized by tumor reduction and induction of apoptosis. Reduction in prostaglandin E2 synthesis also led to reduced level of VEGF in plasma [2].
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2[1].
Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays high affinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06.
Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
L 888607 Racemate is a selective prostaglandin D2 receptor subtype 1 (DP1) antagonist, with Kis of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.
(S)-Butaprost (free acid) is a potent and highly selective agonist of EP2 receptor[1].
Butaprost is a selective prostaglandin E receptor (EP2) agonist with a Ki of 2.4 μM for murine EP2 receptor. Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost effectively mitigates renal fibrogenesis[1][2][3].
CRTh2 antagonist 2 is selective and potent CRTH2 antagonist extracted from patent US20140148470A1, compound Example 1, has an IC50 of ≤10 nM. CRTh2 antagonist 2 can be used in research of androgenic alopecia[1].
Misoprostol(SC29333) is a synthetic prostaglandin E1 (PGE1) analog that is used to prevent gastric ulcers, to treat missed miscarriage, to induce labor, and to induce abortion.Target: Prostaglandin ReceptorMisoprostol is a synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion, and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties. Misoprostol seems to inhibit gastric acid secretion by a direct action on the parietal cells through binding to the prostaglandin receptor. Administration of misoprostol to EP3+/+ and EP3-/- mice showed similar levels of infarct rescue, indicating that misoprostol protection was not mediated through the EP3 receptor. Taken together, these findings suggest a novel function for misoprostol as a protective agent in cerebral ischemia acting via the PGE(2) EP2 and/or EP4 receptors [1, 2].
(8-epi)-BW 245C is the C-8 diastereomer of BW 245C (HY-101987). BW 245 C is a high affinity and selective PGD2 receptor agonist[1].
2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide is a compound that inhibits stress-induced ulcer and low toxicity, and can maintain the content of phospholipase A2 and prostaglandin E2 in ulcerated rats induced by water immersed restrained stress.
Ifetroban (BMS-180291) sodium is an orally active antagonist of thromboxane A2 (TXA2) or prostaglandin H2 (PGH2) receptor. Ifetroban sodium shows antiplatelet activity, and inhibits tumor cell migration without affecting cell proliferation. Ifetroban sodium can be used for myocardial ischemia, hypertension, stroke, thrombosis, cardiomyopathy research[1][2][3][4].
BAY-6672 is a potent and selective human Prostaglandin F (FP) receptor antagonist with an IC50 value of 11 nM.
OBE022 is an oral and selective prostaglandin F2α (PGF2α) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively.
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