2. Academic Validation
  3. 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

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

  • J Med Chem. 2010 Mar 25;53(6):2666-70. doi: 10.1021/jm100022r.
Hong C Shen 1,  Fa-Xiang Ding,  Subharekha Raghavan,  Qiaolin Deng,  Silvi Luell,  Michael J Forrest,  Ester Carballo-Jane,  Larissa C Wilsie,  Mihajlo L Krsmanovic,  Andrew K Taggart,  Kenneth K Wu,  Tsuei-Ju Wu,  Kang Cheng,  Ning Ren,  Tian-Quan Cai,  Qing Chen,  Junying Wang,  Michael S Wolff,  Xinchun Tong,  Tom G Holt,  M Gerard Waters,  Milton L Hammond,  James R Tata,  Steven L Colletti
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories,Merck & Co, Inc, Rahway, New Jersey 07065-0900, USA. mail: [email protected]
PMID: 20184326 DOI: 10.1021/jm100022r
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-10680
    99.43%, GPR109A Agonist