EP4 receptor antagonist 1
- Product Name
- EP4 receptor antagonist 1
- CAS No.
- 2287259-07-6
- Chemical Name
- EP4 receptor antagonist 1
- Synonyms
- EP4 receptor antagonist 1;4-[(1S)-1-[[[4-(1E)-1-propen-1-yl-1-[[4-(trifluoromethyl)phenyl]methyl]-1H-1,2,3-triazol-5-yl]carbonyl]amino]ethyl]-benzoic acid;Benzoic acid, 4-[(1S)-1-[[[4-(1E)-1-propen-1-yl-1-[[4-(trifluoromethyl)phenyl]methyl]-1H-1,2,3-triazol-5-yl]carbonyl]amino]ethyl]-;HEK293,Prostaglandin Receptor,EP4,immunotherapy,Inhibitor,inhibit,EP4 receptor antagonist 1,EP-4 receptor antagonist 1,cells,cancer
- CBNumber
- CB66327039
- Molecular Formula
- C23H21F3N4O3
- Formula Weight
- 458.43
- MOL File
- 2287259-07-6.mol
EP4 receptor antagonist 1 Property
- Density
- 1.32±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
- form
- A crystalline solid
- pka
- 4.19±0.10(Predicted)
- color
- White to off-white
EP4 receptor antagonist 1 Chemical Properties,Usage,Production
Biological Activity
EP4 receptor antagonist 1 is an antagonist of the prostaglandin E2 (PGE2) receptor EP4 that has an IC50 value of 6.1 nM in a calcium flux assay using CHO cells co-expressing the human receptor and Gα16.1 It is selective for EP4 over EP1, EP2, and EP3 receptors (IC50s = >10,000 nM for all). EP4 receptor antagonist 1 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells expressing EP4. It reverses ERK phosphorylation induced by PGE2 in CHO cells expressing EP4 and decreases GM-CSF-induced expression of Il1b, Il4ra, Il6, Arg1, Cox2, and Il10 in RAW 264.7 cells when used at a concentration of 10 μM. EP4 receptor 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.
References
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)
EP4 receptor antagonist 1 Preparation Products And Raw materials
Raw materials
Preparation Products
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