Palupiprant | E-7046 | EP4 Antagonist | AmBeed-信号通路专用抑制剂

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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 3D分子结构
CAS号：1369489-71-3

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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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell Host Microbe, 2024. Ambeed. [ A163338 ]; • Cancer Res., 2024. Ambeed. [ A295334 ]; • J. Pharm. Investig., 2024. Ambeed. [ A221527 , A691302 , A272538 , A187261 ]; • J. Fungi, 2024, 10(11): 751. Ambeed. [ A796919 ]; • JBC, 2024, 107935. Ambeed. [ A194396 ]; 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

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 {[allProObj[0].p_purity_real_show]}

Palupiprant 纯度/质量文件产品仅供科研

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Palupiprant {[allProObj[0].p_purity_real_show]}

Palupiprant 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Palupiprant 质控信息

Palupiprant 生物活性

Palupiprant 临床研究

Palupiprant 参考文献

Palupiprant 实验方案

Palupiprant 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Palupiprant 纯度/质量文件产品仅供科研