TXA₂/TP Antagonist

ONO-AE3-208 is a selective and orally active EP4 receptor antagonist with a K_i of 1.3 nM. ONO-AE3-208 shows less potently affects EP3, FP, and TP receptors (K_i of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 suppresses cell invasion, migration, and metastasis of prostate cancer.

Laropiprant is a potent and selective DP receptor antagonist with K_i values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.

AGN 225660 is a multi-prostanoid receptor antagonist with human IC₅₀ values of 70, 70, 5, 220 and 180 nM for EP1, EP4, TP, DP1, FP. AGN 225660 inhibits secretion of RANTES, IL-8, MCP-1, IL-12p70, and IL-23. AGN 225660 exhibits good ocular bioavailability and reduces ocular inflammation linked to phacoemulsification surgery and uveitis.

TPα/β antagonist-1 is a TXA2 receptor α (TPα) and TPβ antagonist with IC₅₀s of 1.52 nM and 0.79 nM, respectively. TPα/β antagonist-1 inhibits U-46619 (HY-108566)-induced intracellular calcium mobilization, and imhibits platelet aggregation. TPα/β antagonist-1 can be used for the research of cardiovascular disease.

Seratrodast (AA 2414), an orally active antiasthmatic agent, is a thromboxane A2 receptor (TP) antagonist and ferroptosis inhibitor. Seratrodast reduces lipid ROS production, modulates the systemic xc-/GSH/GPX4 axis, and inhibits JNK phosphorylation and p53 expression. Seratrodast exhibits anti-asthmatic and anti-epileptic activity.

Ramatroban is a selective thromboxane A₂ (TxA₂, IC₅₀=14 nM) antagonist, which also antagonizes CRTH2 (IC₅₀=113 nM) by inhibiting PGD₂ binding.

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).

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.

L 888607 Racemate is a selective prostaglandin D₂ receptor subtype 1 (DP1) antagonist, with K_is of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.

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.

MK-7246 is a potent and selective CRTH2 antagonist with a K_i of 2.5±0.5 nM.

Ifetroban (BMS-180291) is an orally active antagonist of thromboxane A2 (TXA2) or prostaglandin H2 (PGH2) receptor. Ifetroban shows antiplatelet activity, and inhibits tumor cell migration without affecting cell proliferation. Ifetroban can be used for myocardial ischemia, hypertension, stroke, thrombosis, cardiomyopathy research.

KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.

TP receptor antagonist-3 (compound 51280) is a potent thromboxane A2 prostanoid (TP) receptor with an IC₅₀ of 15.7 nM against Human TP. TP receptor antagonist-3 can be used for alzheimer's disease, cardiovascular and respiratory diseases, and cancer research.

SC 51089 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 exhibits neuroprotective activity.

Sulotroban (SKF-95587; BM-13177) is a selective antagonist for thromboxane A2 receptor (TXA2 Receptor). Sulotroban exhibits inhibitory activity against carbocyclic thromboxane A2- and endoperoxide-induced vasoconstrictor. Sulotroban inhibits platelets aggregation.

Laropiprant sodium is a potent and selective DP receptor antagonist with K_i values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.

ICI 185282 is a potent, selective, orally active thromboxane A2 (TXA₂) receptor antagonist. ICI 185282 causes dose-dependent inhibition of U-46619 (HY-108566)-induced platelet aggregation ex-vivo in guinea-pig. ICI 185,282 inhibits bronchospasm induced by U-46619, PGD₂ (HY-101988), PGF_2α (HY-12956), arachidonic acid (HY-109590), LTD₄ and PAF (HY-108635) in vivo. ICI 185282 can be used for bronchial asthma research.

(S)-Trimetoquinol hydrochloride (Compound 1) is a apotent, nonselective, nonclassical β-adrenergic agonist and nonprostanoid thromboxane A2/prostaglandin H2 antagonist. (S)-Trimetoquinol hydrochloride can be used for research of neurological and cardiovascular disease.

CGS 22652 is a potent thromboxane A2 receptor antagonist. CGS 22652 has selective thromboxane A2 synthase inhibitory properties. CGS 22652 can be used in the research of coronary artery thrombosis.