E7046

    
99%

E7046

源叶(MedMol)
S83013 一键复制产品信息
1369489-71-3
C22H18F5N3O4
483.388036
E7046; E-7046; E 7046
货号 规格 价格 上海 北京 武汉 南京 购买数量
S83013-5mg 99% ¥250.00 5 - - -
S83013-10mg 99% ¥370.00 6 - - -
S83013-25mg 99% ¥630.00 6 - - -
S83013-100mg 99% ¥1720.00 货期:2-3天 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

Palupiprant (E7046) is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. Palupiprant exhibits anti-tumor activities

产品描述: Palupiprant (E7046) is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. Palupiprant exhibits anti-tumor activities
靶点: IC50: 13.5 nM (EP4) Ki: 23.14 nM (EP4);ProstaglandinReceptor
体外研究: Palupiprant (E7046) reverses the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells through selective EP4 antagonism。
体内研究: In the CT-26 tumor model, the E7046/RT combination causes the anti-tumor memory response of 9 animals. In the 4T1 model, the combination of E7046 and RT also produces significant better tumor growth inhibition activity compared with each treatment alone. The combination significantly improves survival by inhibiting the subsequent spontaneous lung metastasis of 4T1 tumors. E7046 (150 mg/kg) inhibits the growth of multiple syngeneic tumor models. Blockade of EP4 signaling promotes anti-tumor DC differentiation and slows tumor growth in mice. E7046 treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8C T cells. Furthermore, co-administration of E7046 and E7777, an IL-2-diphtheria toxin fusion protein that preferentially kills Tregs, synergistically disrupts the myeloid and Treg immunosuppressive networks, resulting in effective and durable anti-tumor immune responses in mouse tumor models.
参考文献: 1. X. Bao, et al. Combination of a Novel EP4 Antagonist E7046 and Radiation Therapy Promotes Anti-tumor Immune Response and Tumor Rejection in Preclinical Tumor Models. International Journal of Radiation Oncology Biology Physics 2. Diana I. Albu, 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.
溶解性: Soluble  in  DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.069 ml 10.344 ml 20.687 ml
5 mM 0.414 ml 2.069 ml 4.137 ml
10 mM 0.207 ml 1.034 ml 2.069 ml
50 mM 0.041 ml 0.207 ml 0.414 ml
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参考文献

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