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Discovery of a Potent and Selective Free Fatty Acid Receptor 1 Agonist With Low Lipophilicity and High Oral Bioavailability

Discovery of a Potent and Selective Free Fatty Acid Receptor 1 Agonist With Low Lipophilicity and High Oral Bioavailability

Elisabeth Christiansen, Maria E Due-Hansen, Christian Urban, Manuel Grundmann, Johannes Schmidt, Steffen V F Hansen, Brian D Hudson, Mohamed Zaibi, Stine B Markussen, Ellen Hagesaether, Graeme Milligan, etc.

J Med Chem. 2013 Feb 14;56(3):982-92.

PMID: 23294321

Abstract:

The free fatty acid receptor 1 (FFA1, also known as GPR40) mediates enhancement of glucose-stimulated insulin secretion and is emerging as a new target for the treatment of type 2 diabetes. Several FFA1 agonists are known, but the majority of these suffer from high lipophilicity. We have previously reported the FFA1 agonist 3 (TUG-424). We here describe the continued structure-activity exploration and optimization of this compound series, leading to the discovery of the more potent agonist 40, a compound with low lipophilicity, excellent in vitro metabolic stability and permeability, complete oral bioavailability, and appreciable efficacy on glucose tolerance in mice.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1082058998	TUG-424		1082058-99-8	Price

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