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EP4 Receptor Antagonist 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EP4 Receptor Antagonist 1图片
CAS NO:2287259-07-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
EP4 受体拮抗剂 1 是一种用于癌症免疫治疗的高效和选择性竞争性前列腺素 EP4 受体拮抗剂。
Cas No.2287259-07-6
Canonical SMILESC[C@@H](C1=CC=C(C=C1)C(O)=O)NC(C2=C(/C=C/C)N=NN2CC3=CC=C(C(F)(F)F)C=C3)=O
分子式C23H21F3N4O3
分子量458.4
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

EP4receptor antagonist 1 is an antagonist of the prostaglandin E2(PGE2) receptor EP4that has an IC50value of 6.1 nM in a calcium flux assay using CHO cells co-expressing the human receptor and Gα16.1It is selective for EP4over EP1, EP2, and EP3receptors (IC50s = >10,000 nM for all). EP4receptor antagonist 1 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells expressing EP4. It reverses ERK phosphorylation induced by PGE2in CHO cells expressing EP4and decreases GM-CSF-induced expression ofIl1b,Il4ra,Il6,Arg1,Cox2, andIl10in RAW 264.7 cells when used at a concentration of 10 µM. EP4receptor antagonist 1 (50 and 150 mg/kg once per day) reduces tumor volume and increases infiltration of CD8+T cells into tumors in a murine colon carcinoma model.

1.Yang, J.-J., Yu, W.-W., Hu, L.-L., et al.Discovery and characterization of 1 H-1,2,3-triazole derivatives as novel prostanoid EP4 receptor antagonists for cancer immunotherapyJ. Med. Chem.63(2)569-590(2020)