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
EP4 receptor antagonist 1 Suppliers
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9805
- Advantage
- 58
- Tel
- 021-QQ：65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 7312
- Advantage
- 58
- Tel
- 021-2022843681 15618226720
- Fax
- +86-21-51601218
- lucy@atkchemical.com
- Country
- China
- ProdList
- 9987
- Advantage
- 58
- Tel
- 0519-85788828 13775037613
- sales@chemrenpharm.com
- Country
- China
- ProdList
- 3600
- Advantage
- 58
- Tel
- 13348960310 13348960310
- 3003867561@qq.com
- Country
- China
- ProdList
- 10524
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- 2625930290@qq.com
- Country
- China
- ProdList
- 6973
- Advantage
- 58
- Tel
- 4008200310
- marketing@tsbiochem.com
- Country
- China
- ProdList
- 24644
- Advantage
- 58
- Tel
- 025-58851786 17714337195
- sales@tybiochem.com
- Country
- China
- ProdList
- 6828
- Advantage
- 58
- Tel
- 021-59167510 18117107507
- vip@med-life.cn
- Country
- China
- ProdList
- 4997
- Advantage
- 58
- Tel
- 025-85560043 15850508050
- Fax
- 025-85563444
- cindy.huang@synzest.com
- Country
- China
- ProdList
- 12000
- Advantage
- 58
- Tel
- 4008-099-669
- 23419001name@qq.com
- Country
- CHINA
- ProdList
- 73043
- Advantage
- 58
- Tel
- sangon@qq.com
- Country
- CHINA
- ProdList
- 47239
- Advantage
- 58
- Tel
- +undefined-21-51877795
- Fax
- +86 21 5161 9052/ 5187 7796
- ivan@atkchemical.com
- Country
- China
- ProdList
- 32965
- Advantage
- 60
- Tel
- --
- Fax
- --
- info@neobioscience.com
- Country
- CHINA
- ProdList
- 6682
- Advantage
- 58
- Tel
- --
- Fax
- --
- chenjw@absin.cn
- Country
- CHINA
- ProdList
- 6705
- Advantage
- 58
- Tel
- --
- Fax
- --
- Proteintech-CN@ptglab.com
- Country
- CHINA
- ProdList
- 6290
- Advantage
- 58