obeticholic-acid and Diabetes-Mellitus

obeticholic-acid has been researched along with Diabetes-Mellitus* in 1 studies

Other Studies

1 other study(ies) available for obeticholic-acid and Diabetes-Mellitus

Article	Year
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. Journal of medicinal chemistry, 2009, Dec-24, Volume: 52, Issue:24 In the framework of the design and development of TGR5 agonists, we reported that the introduction of a C(23)(S)-methyl group in the side chain of bile acids such as chenodeoxycholic acid (CDCA) and 6-ethylchenodeoxycholic acid (6-ECDCA, INT-747) affords selectivity for TGR5. Herein we report further lead optimization efforts that have led to the discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a novel potent and selective TGR5 agonist with remarkable in vivo activity. Topics: Animals; Chlorocebus aethiops; CHO Cells; Cholic Acids; COS Cells; Cricetinae; Cricetulus; Diabetes Mellitus; Humans; Obesity; Rats; Receptors, G-Protein-Coupled; Stereoisomerism	2009

Article

Year

Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.

Journal of medicinal chemistry, 2009, Dec-24, Volume: 52, Issue:24

In the framework of the design and development of TGR5 agonists, we reported that the introduction of a C(23)(S)-methyl group in the side chain of bile acids such as chenodeoxycholic acid (CDCA) and 6-ethylchenodeoxycholic acid (6-ECDCA, INT-747) affords selectivity for TGR5. Herein we report further lead optimization efforts that have led to the discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a novel potent and selective TGR5 agonist with remarkable in vivo activity.

Topics: Animals; Chlorocebus aethiops; CHO Cells; Cholic Acids; COS Cells; Cricetinae; Cricetulus; Diabetes Mellitus; Humans; Obesity; Rats; Receptors, G-Protein-Coupled; Stereoisomerism

2009