For research use only. Not for therapeutic Use.
GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
GPR40 agonist 4 tends to have a low risk of activating caspase-3/7[1].
Single oral administration of GPR40 agonist 4 (compound 20) robustly reduces the plasma glucose excursion and enhances insulin secretion during an oral glucose tolerance test (OGTT) in a dose-dependent manner from 1 to 10 mg/kg when GPR40 agonist 4 is dosed 60 min prior to the oral glucose challenge. The area under the curve of blood glucose (AUC0-120min) and blood insulin (AUC0-120min) reveal that the minimum effective dose of GPR40 agonist 4 is 3 mg/kg. The hyperglycemia state is also markedly improved in GPR40 agonist 4 (20 mg/kg) treated group[1].
| Catalog Number | I014460 |
| CAS Number | 2102196-57-4 |
| Synonyms | 2-[4-[[3-(2-chlorophenyl)phenyl]methoxy]phenyl]sulfonylacetic acid |
| Molecular Formula | C21H17ClO5S |
| Purity | ≥95% |
| InChI | InChI=1S/C21H17ClO5S/c22-20-7-2-1-6-19(20)16-5-3-4-15(12-16)13-27-17-8-10-18(11-9-17)28(25,26)14-21(23)24/h1-12H,13-14H2,(H,23,24) |
| InChIKey | YEFZZALZTNOYEA-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C(=C1)C2=CC=CC(=C2)COC3=CC=C(C=C3)S(=O)(=O)CC(=O)O)Cl |
| Reference | [1]. Li Z, et al. Discovery of phenylsulfonyl acetic acid derivatives with improved efficacy and safety as potent free fatty acid receptor 1 agonists for the treatment of type 2 diabetes. Eur J Med Chem. 2017 Sep 29;138:458-479. |
