| Bioactivity | GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54. | ||||||||||||
| Target | pEC50: 7.54 (FFA1/GPR40) | ||||||||||||
| Invitro | GPR40 agonist 4 tends to have a low risk of activating caspase-3/7[1]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | GPR40 agonist 4 | ||||||||||||
| CAS | 2102196-57-4 | ||||||||||||
| Formula | C21H17ClO5S | ||||||||||||
| Molar Mass | 416.87 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |