|Solubility:||DMSO up to 50 mM|
|Chemical Name:||3-(2-fluoro-4-(((1-(2-phenoxyethyl)-1,2,3,4-tetrahydroquinolin-5-yl)methyl)amino)phenyl)propanoic acid|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
AS2034178 is the potent, selective and orally bioavailable GPR40 (FFA1) agonist. It has good selectivity for over GPR41, GPR43, GPR119, GPR120 and PPARγ. It can Induce glucose-dependent insulin secretion in pancreatic MIN6 cells and in vivo. AS2034178 could decrease plasma glucose and HbA1c levels after repeat administration to ob/ob mice, with favorable oral absorption and pharmacokinetics. Repeat administration of AS2034178 enhanced insulin sensitivity in an insulin tolerance test and a euglycemic-hyperinsulinemic clamp test.
How to Use:
In vitro: AS2034178 was used at 1-10 µM final concentration in various in vitro assays.
In vivo: AS2034178 was dosed to normal mice and Zucker fatty rats under fasting conditions for oral glucose tolerance test via oral gavage at 3-10 mg/kg. It was dosed to diabetic ob/ob mice via oral gavage at 3-30 mg/kg once per day for 2 weeks.
- Tanaka H, et al. Chronic treatment with novel GPR40 agonists improve whole-body glucose metabolism based on the glucose-dependent insulin secretion. (2013) J Pharmacol Exp Ther. 346(3):443-52.
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