Prostaglandin Receptor Antagonist

ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with K_i value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer.

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.

AZD1981 is the antagonist for GPR44 (also known also PTGDR2, DP2 or CRTh). AZD1981 blocks the binding of PGD2 to CRTH2. AZD1981 exhibits immunomodulatory effects and can be used in research of chronic spontaneous urticaria.

Terutroban (S-18886) is a selective and orally active thromboxane-prostaglandin (TP) receptor antagonist with an IC₅₀ of 16.4 nM. Terutroban inhibits TXA2 and prostaglandin endoperoxide receptors. Terutroban is a potent antithrombotic agent and possesses anti-atherosclerotic and anti-vasoconstrictor properties.

AL-8810 is a potent and selective antagonist of the PGF _2α receptor (FP receptor). AL-8810 is an activator of MAPK and ERK1/2. The K_i of the FP receptor of mouse 3T3 cells and rat A7r5 cells are 0.2±0.06 μM and 0.4±0.1 μM, respectively. AL-8810 can be used in the study of elevated intraocular pressure (OHT) and primary open-angle glaucoma (POAG).

SQ 29548 is a selective thromboxane-prostanoid (TP) receptor antagonist.

MF498 is a selective and orally active E prostanoid Receptor 4 (EP4) antagonist with a K_i value of 0.7 nM. MF498 can be used in the research of inflammation, such as rheumatoid and osteoarthritis.

NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC₅₀ of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca²⁺] mobilization following stimulation of cells with the alternative TP agonist U46619. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH).

MF-766 is a highly potent, selective and orally active EP4 antagonist with a K_i of 0.23 nM. MF-766 behaves 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. MF-766 can be used for cancer and inflammation diseases research.

MK-2894 is a potent, selective, orally active and high affinity (K_i=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC₅₀=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis.

Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC₅₀s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment.

SC 51089 free base is a selective antagonist of prostaglandin E₂ EP1 receptor, with K_is 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.

TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. TG8-260 can reduce neuroinflammation and gliosis in the hippocampus of rats after pilocarpine-induced persistent epileptic status. Pharmacokinetic data of TG8-260 showed that its plasma half-life was 2.14 hours and its oral bioavailability was 77.3%. TG8-260 is also a potent inhibitor of CYP450 and shows antagonistic activity in inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia, which is suitable for studying anti-inflammatory pathways in animal models of peripheral inflammatory diseases.

BW A868C, a hydantoin compound, is a BW245C structural analogue. BW A868C is a selective and potent competitive prostaglandin D2 (PGD2) antagonist. BW A868C has no effect on other prostaglandin receptors (IP, EP1, EP2, TP and FP).

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.

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.

EP3 antagonist 3 (compound 2) is an orally active, potent and selective EP3 antagonist, with a pK_i of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research.

L-826266 is a selective and competitive EP3 receptor antagonist. L-826266 can be used for convulsive disorders research.

EP2 receptor antagonist-3 is a selective EP2 receptor antagonist (IC₅₀: 8 nM in hEP2 SPA assay, 50 nM in hEP2 cAMP assay). EP2 receptor antagonist-3 increases the macrophage-mediated clearance of Amyloid-β plaques. EP2 receptor antagonist-3 can be used for the study of alzheimer’s diseases.

Ebopiprant (OBE022) is an oral and selective prostaglandin F_2α (PGF_2α) receptor antagonist, with K_is of 1 nM, 26 nM for human and rat FP receptors, respectively.