S85388 |
GW627368 |
| 源叶(MedMol) | ≥98%(HPLC) |
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- 产品描述： 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
- 靶点： EP
- 体外研究： GW627368 (GW627368X) appears to bind to human prostanoid TP receptors but not the TP receptors of other species. GW627368 (GW627368X) (10 μM) produces 100% inhibition of U-46619 (EC100)-induced aggregation (approximate pA2 approximately 7.0) in human washed platelets. 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. 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
- 体内研究： 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. Animal Model: 6-8 weeks Swiss albino mice Dosage: 0 mg/kg, 5 mg/kg, 10 mg/kg, 15 mg/kg, 15 mg/kg Administration: Oral administration, every alternate day for 28 days Result: Displayed anti-tumor and anti-proliferative potential in sarcoma 180 bearing mice.
- 参考文献：
1. Wilson RJ, et al. GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist. Br J Pharmacol. 2006 Jun;148(3):326-39. 2. Robertson FM, et al. Molecular and pharmacological blockade of the EP4 receptor selectively inhibits both proliferation and invasion of human inflammatory breast cancer cells. J Exp Ther Oncol. 2008;7(4):299-312. 3. Parida S, et al. Molecular inhibition of prostaglandin E2 with GW627368X: Therapeutic potential and preclinical safety assessment in mouse sarcoma model. Cancer Biol Ther. 2015;16(6):922-32.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.836 ml 9.181 ml 18.361 ml 5 mM 0.367 ml 1.836 ml 3.672 ml 10 mM 0.184 ml 0.918 ml 1.836 ml 50 mM 0.037 ml 0.184 ml 0.367 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
