CAS NO: | 2287259-07-6 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
Cas No. | 2287259-07-6 |
Canonical SMILES | C[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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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) |