Network Version
| Product Name: | GW627368 |
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| CAS No.: | 439288-66-1 | |
| Cat. No.: | HY-16963 | |
| MWt: | 544.62 | |
| Formula: | C30H28N2O6S | |
| Purity : | >98% | |
| Solubility: | DMSO : 100 mg/mL (183.61 mM; Need ultrasonic) | |
| Mechanisms: | Target: Cancer Endocrinology Inflammation/Immunology | |
| Biological Activity: | ||
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GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor with additional human TP receptor affinity, with pKi 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]. |
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