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J Med Chem. 2010 Mar 25;53(6):2666-70. doi: 10.1021/jm100022r.

Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories,Merck & Co, Inc, Rahway, New Jersey 07065-0900, USA. mail: hong_shen@merck.com

Abstract

Biaryl cyclohexene carboxylic acids were discovered as full and potent niacin receptor (GPR109A) agonists. Compound 1e (MK-6892) displayed excellent receptor activity, good PK across species, remarkably clean off-target profiles, good ancillary pharmacology, and superior therapeutic window over niacin regarding the FFA reduction versus vasodilation in rats and dogs.

PMID:
20184326
DOI:
10.1021/jm100022r
[Indexed for MEDLINE]

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