E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM, exhibiting anti-tumor activities.
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 U46609[1]. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH)[2].
ER-819762 is a novel potent, selective, orally active EP4 receptor antagonist with IC50 of 59 nM in cAMP-dependent reporter assay; inhibits EP4-stimulated Th1 differentiation, Th17 cell expansion, and IL-23 secretion by activated dendritic cells; exhibits no agonism or antagonism for the related PGE2 EP1, EP2 and EP3 receptors; suppresses Th1 and Th17 cytokine production, suppresses disease in collagen- and GPI-induced arthritis in mice, and suppresses CFA-induced inflammatory pain in rats.
KW-8232 free base is an anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.
Tiaprost is a prostaglandin F2α (PGF2α) analogue.
L-798106 is potent and highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM), it also has micromolar activities at the EP4, EP1 and EP2 receptors with Ki values of 916 nM, >5000 nM and >5000 nM at EP4, EP1 and EP2, respectively[1].
Evatanepag (CP-533536) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.IC50 value: 0.3 nM (EC50)Target PGE2in vitro: CP-533536 is a potent and selective EP2agonist. CP-533536 demonstrates the ability to heal fractures when administered locally as a single dose in rat models of fracture healing. CP-533536 demonstrates excellent in vitro potency against EP2 and selectivity against a broad panel of other targets.
Aligeron is a non-selective prostaglandin (PG) antagonist, and has vasodilatory properties.
trans-Isoferulic acid (trans-3-Hydroxy-4-methoxycinnamic acid) is an aromatic acid isolated from the roots of Clematis florida var. plena. trans-Isoferulic acid exhibits anti-inflammatory activity[1].trans-isoferulic acid suppresses NO and PGE2 production through the induction of Nrf2-dependent heme oxygenase-1 (HO-1)[2].
Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.
MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.
MK-2894 is a highly potent and selective second generation EP4 antagonist.IC50 value:Target: EP4MK-2894 exhibits favorable pharmacokinetic profile in a number of preclinical species and potent anti-inflammatory activity in several animal models of pain/inflammation. MK-2894 also shows favorable GI tolerability profile in rats when compared to traditional NSAID indomethacin.
Etersalate inhibits platelet function and decreases thromboxane A2 (TXA2) levels.
Ethamsylate is a haemostatic drug, also inhibits biosynthesis and action of those prostaglandins.
U-46619 (9,11-Methanoepoxy PGH2) is a stable analogue of thromboxane A2 (TXA2) and acts as a potent TXA2 agonist[1].
TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM[1][2]. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1[1]. TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor[2].
Laropiprant sodium is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively[1][2][3].
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor[1].
LAS191859 is an orally active, potent and selective CRTh2 antagonist with an IC50 of 9.58 nM against human CRTh2. LAS191859 can be used for the research of chronic asthma[1].
Ginsenoside Ro exhibits a Ca2+-antagonistic antiplatelet effect with an IC50 of 155 μM. Ginsenoside Ro reduces the production of TXA2 more than it reduces the activities of COX-1 and TXAS.
Prostaglandin D3 (PGD3) is a prostaglandin that acts as an inhibitor of platelet aggregation and a modulator of autonomic neurotransmission in humans[1].
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM)[1].
Iloprost (ZK 36374) is a synthetic analogue of prostacyclin PGI2.Target: Iloprost is a stable prostacyclin analog commonly employed in the treatment of peripheral vascular disease and also indicated in the treatment of patients affected by systemic sclerosis (SSc) in the presence of severe Raynaud's phenomenon (RP). [1] Iloprost dilates systemic and pulmonary arterial vascularbeds. Iloprost also affects platelet aggregation but the relevance of this effect to the treatment of pulmonary hypertension is unknown. The two diastereoisomers of iloprost differ in their potency in dilating blood vessels, with the 4S isomer substantially more potent than the 4R isomer.[2] Iloprost is a stable carbacyclin derivative of prostacyclin, was studied during electrically-induced coronary artery thrombosis in the open chest anesthetized pig. Infusion of ZK 36374 (100 ng/kg/min, n = 6) had no effect on heart rate and cardiac output, but caused a 20% reduction in mean arterial blood pressure by peripheral vasodilation. In animals receiving solvent or no drug prior to thrombosis induction, the time to occlusive coronary artery thrombosis (TOT) was 30 +/- 2 minutes (mean +/- SEM, n = 17). Pretreatment with an i.v. infusion of ZK 36374 (100 ng/kg/min) prolonged TOT by 50% to 47 +/- 7 minutes (p less than 0.005, n = 6). This prolongation of TOT was not due to the lower blood pressure in the ZK 36374 group, as dihydralazine in a dose that lowered arterial blood pressure to the same extent had no effect on TOT (32 +/- 4 minutes, n = 4). The results indicate that ZK 36374 may be useful in delaying (or preventing) occlusive coronary artery thrombi. [3]
SC 34301 (Enisoprost) is a potent and orally active PGE1 analog. SC 34301 significantly reduces bacterial translocation and improves survival for burned mice[1][2].
Dinoprost(Prostaglandin F2α) is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC50 value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels[1].
ONO-AE3-208 is an EP4 antagonist, and suppresses cell invasion, migration, and metastasis of prostate cancer.
SQ 26655 is a TxA2 receptor agonist. SQ 26655 induces human platelet aggregation[1].
Dazoxiben is a potent and orally active thromboxane (TX) synthase inhibitor[1].
BMY 45778 is a non-prostanoid prostacyclin mimetic. BMY 45778 inhibits human (IC50 = 35 nM), rabbit (IC50: 136 nM) and rat (IC50 : 1.3 μM) platelet aggregation. BMY 45778 also activates adenylyl cyclase. BMY 45778 is a partial agonist at the prostacyclin receptor[1].