MK-0354

MK-0354 is an orally administered small molecule drug that acts as a partial agonist of the GPR109a receptor (also known as Hydroxycarboxylic acid receptor 2 or Niacin receptor 1). It was developed for the treatment of atherosclerosis and related disorders by targeting G protein-coupled receptors involved in regulating plasma lipid profiles—particularly HDL cholesterol—similar to the mechanism of niacin. Unlike niacin itself, MK-0354 exhibits antilipolytic activity without causing vasodilation in preclinical models. The compound contains a tetrazole moiety that mimics the carboxylic acid group of niacin but results in weaker efficacy due to altered receptor interactions. Development reached phase II clinical trials for dyslipidemia and atherosclerosis but was discontinued[2][3][8].

Other names

851776-28-83-(2H-tetrazol-5-yl)-1,4,5,6-tetrahydrocyclopenta[c]pyrazole