FAA1agonist-1是一个强效的游离脂肪酸受体1(FFA1/GPR40)激动剂，其pEC50值为7.54。
CAS：2102196-57-4
分子式：C21H17ClO5S
分子量：416.87
纯度：98%
存储：Store at -20°C

Background:

FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.

FAA1 agonist-1 (compound 20) (10 mg/kg) presents superior pharmacokinetic (PK) profiles, in particular, a high maximum concentration (Cmax=2563.52 μg/L), low clearance (CL=0.154 L/h/kg), long plasma half-life (T1/2=5.57 h) and results in a high exposure (AUC0-24h=30204.43 μg/L•h). FAA1 agonist-1 also tends to have a low risk of activating caspase-3/7[1].

Single oral administration of FAA1 agonist-1 (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 FAA1 agonist-1 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 FAA1 agonist-1 is 3 mg/kg. The hyperglycemia state is also markedly improved in FAA1 agonist-1 (20 mg/kg) treated group[1].

[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.