GW627368

GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor with additional human TP receptor affinity, with pK_i values of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively^[1]. IC50 & Target: pKi ：7.0 (hEP4), 6.8 (hTP)^[1] In Vitro: GW627368 (GW627368X) appears to bind to human prostanoid TP receptors but not the TP receptors of other species^[1].
GW627368 (GW627368X) (10 μM) produces 100% inhibition of U-46619 (EC₁₀₀)-induced aggregation (approximate pA2 approximately 7.0) in human washed platelets^[1].
GW627368 (GW627368X) is devoid of agonist activity and actually produced a significant and concentration-related reduction in basal cAMP levels with pIC₅₀ value of 6.3^[1].
GW627368 (GW627368X) induces inhibition of proliferation and invasion of human SUM149 IBC tumor cells beginning at 0.1 μM, with inhibition of proliferation and invasion of MDA-MB-231 non-IBC cells at higher concentrations^[2].
In Vivo: GW627368 (GW627368X) (0-15 mg/kg; p.o.; every alternate day for 28 days) shows significant tumor regression characterized by tumor reduction and induction of apoptosis^[3].