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 | Health & Environmental Research Online (HERO)

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Citation
Tags

HERO ID

7209866

Reference Type

Journal Article

Title

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

Author(s)

Pellicciari, R; Gioiello, A; Macchiarulo, A; Thomas, C; Rosatelli, E; Natalini, B; Sardella, R; Pruzanski, M; Roda, A; Pastorini, E; Schoonjans, K; Auwerx, J; ,

Year

2009

Is Peer Reviewed?

Yes

Journal

Journal of Medicinal Chemistry
ISSN: 0022-2623
EISSN: 1520-4804

Language

English

PMID

20014870

DOI

10.1021/jm901390p

Abstract

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.