1208866-49-2Relevant academic research and scientific papers
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
Shen, Hong C.,Ding, Fa-Xiang,Raghavan, Subharekha,Deng, Qiaolin,Luell, Silvi,Forrest, Michael J.,Carballo-Jane, Ester,Wilsie, Larissa C.,Krsmanovic, Mihajlo L.,Taggart, Andrew K.,Wu, Kenneth K.,Wu, Tsuei-Ju,Cheng, Kang,Ren, Nina,Cai, Tian-Quan,Chen, Qing,Wang, Junying,Wolff, Michael S.,Tong, Xinchun,Holt, Tom G.,Waters, M.Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
supporting information; experimental part, p. 2666 - 2670 (2010/08/22)
Biaryl cyclohexene carboxylic acids were discovered as full and potent niacin receptor (GPR 109A) 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.
Niacin receptor agonists, compositions containing such compounds and methods of treatment
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Page/Page column 24; 44, (2010/11/25)
The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
