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.
CAS Number: 1030846-42-4
Molecular Weight: 448.53
Chemical Name: 3-(2-fluoro-4-(((1-(2-phenoxyethyl)-1,2,3,4-tetrahydroquinolin-5-yl)methyl)amino)phenyl)propanoic acid
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
AS2034178 was used at 1-10 µM final concentration in various in vitro assays.
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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