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Biological Activity:

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.

Reference:

1.  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. 

Products are for research use only. Not for human use.