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首页-小分子抑制剂&激动剂-GPCR-Prostaglandin Receptor-E7046
E7046

Chemical Structure : E7046

CAS No.: 1369489-71-3

E7046 (Palupiprant, ER-886046)

货号: PC-63545Not For Human Use, Lab Use Only.

E7046 (Palupiprant, ER-886046) is a potent, selective, orally bioavailable EP4 receptor antagonist with IC50 of 13.5 nM, Ki of 23.14 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

E7046 (Palupiprant, ER-886046) is a potent, selective, orally bioavailable EP4 receptor antagonist with IC50 of 13.5 nM, Ki of 23.14 nM.
E7046 (Palupiprant, ER-886046) displays >1,500 fold selectivity for EP4 relative to EP4 closest homolog, the PGE2 receptor EP2.
E7046 (Palupiprant, ER-886046) diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity.
E7046 (Palupiprant, ER-886046) shows anti-arthritic potential in collagen induced arthritis model.

物理化学性质&存储条件

分子量 483.395
分子式 C22H18F5N3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-4-(1-(3-(difluoromethyl)-1-methyl-5-(3-(trifluoromethyl)phenoxy)-1H-pyrazole-4-carboxamido)ethyl)benzoic acid

参考文献

1. Bender AT, et al. Am J Transl Res. 2013;5(1):92-102.

2. Albu DI, et al. Oncoimmunology. 2017 Jun 28;6(8):e1338239.

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