产品说明书
Palupiprant
 |
同义名 : | E-7046;ER-886406;Palupiprantum;AN0025 |
| CAS号 : | 1369489-71-3 | |
| 货号 : | A368414 | |
| 分子式 : | C22H18F5N3O4 | |
| 纯度 : | 99%+ | |
| 分子量 : | 483.388 | |
| MDL号 : | MFCD30502665 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(217.22 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The EP4 prostanoid receptor is one of four receptor subtypes for prostaglandin E2, which belongs to the family of G protein-coupled receptors. EP4 signaling plays a variety of roles through cAMP effectors, i.e., protein kinase A and exchange protein activated by cAMP[1]. E7046 is a newly developed and highly specific EP4 antagonist with IC50 of 13.5 nM and with a >1500 fold selectivity for EP4 relative to the PGE2 receptor EP2. E7046 reversed the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells through selective EP4 antagonism. In murine BM-derived haematopoietic cells induced to differentiate into CD11c-expressing DCs, E7046 antagonism of PGE2 effects on BM cell differentiation rescued T cell proliferation in response to TCR activation in a dose-dependent manner. Daily oral administration of 150 mg/kg E7046 was found to inhibit the growth of multiple syngeneic tumor models: fibrosarcoma SaI/N, pancreatic PAN02, colon CT26, and breast EMT6 and 4T1[2]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03152370 | Neoadjuvant Therapy in Rectal ... 展开 >>Cancer 收起 << | Phase 1 | Recruiting | January 2019 | United States, Massachusetts ... 展开 >> Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 United States, New York Weill Cornell Recruiting New York, New York, United States, 10065 Poland Marie-Skodowska Curie Cancer Centre Recruiting Warsaw, Poland United Kingdom The Christie Recruiting Manchester, United Kingdom Mount Vernon Hospital Recruiting Northwood, United Kingdom 收起 << |
| NCT02540291 | Tumors | Phase 1 | Terminated(Terminated due to, ... 展开 >>licensing agreement granting exclusive rights of research, development, manufacture and marketing of Eisai's E7046 to Adlai Nortye Biopharma.) 收起 << | - | United States, Massachusetts ... 展开 >> Boston, Massachusetts, United States United States, Texas Houston, Texas, United States France Villejuif, Cedex, France 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.07mL 0.41mL 0.21mL |
10.34mL 2.07mL 1.03mL |
20.69mL 4.14mL 2.07mL |
| 参考文献 |
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