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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / 前列腺素受体 / Palupiprant

Palupiprant {[allProObj[0].p_purity_real_show]}

货号：A368414 同义名： E-7046;ER-886406

E7046 is a specific antagonist of the type 4 prostaglandin E2 (PGE2) receptor EP4. It possesses significant antitumor growth activity in multiple preclinical tumor models through modulating myeloid cells, including tumor-associated macrophages and myeloid-derived suppressor cells.

Palupiprant 化学结构 CAS号：1369489-71-3
Palupiprant 化学结构
CAS号：1369489-71-3
Palupiprant 3D分子结构
CAS号：1369489-71-3
Palupiprant 化学结构 CAS号：1369489-71-3
Palupiprant 3D分子结构 CAS号：1369489-71-3
规格 价格 会员价 库存 数量
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Palupiprant 纯度/质量文件 产品仅供科研

货号：A368414 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]
• JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]
• BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]
• J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]
• PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]
更多 >

Palupiprant 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].

Palupiprant 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 <<

Palupiprant 参考文献

[1]Yokoyama U, Iwatsubo K, Umemura M, Fujita T, Ishikawa Y. The prostanoid EP4 receptor and its signaling pathway. Pharmacol Rev. 2013;65(3):1010-1052. Published 2013 Jun 17.

[2]Albu DI, Wang Z, Huang KC, et al. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. Oncoimmunology. 2017;6(8):e1338239. Published 2017 Jun 28.

Palupiprant 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.34mL

2.07mL

1.03mL

20.69mL

4.14mL

2.07mL

Palupiprant 技术信息

CAS号1369489-71-3
分子式C22H18F5N3O4
分子量 483.388
别名 E-7046;ER-886406;Palupiprantum;AN0025
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
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
动物实验配方

Tags: Palupiprant | 1369489-71-3 | E7046 | E 7046 | E-7046 | EP4 Antagonist | GPCR/G Protein | Prostaglandin Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Palupiprant 纯度/质量文件 | Palupiprant 生物活性 | Palupiprant 临床数据 | Palupiprant 参考文献 | Palupiprant 实验方案 | Palupiprant 技术信息

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