Description
MK-0354 is a potent, selective niacin receptor GPR109A partial agonist with EC50 of 1.65 and 1.08uM for hGPR109A andmgPR109A in the whole cell cAMP assays; shows no interaction with any other target in a panel of over 120 other proteins; MK-0354 is a competitive inhibitor of 3H-nicotinic acid binding to hGPR109a with Ki of 505nM, fully inhibits isoproterenol stimulated lipolysis in human adipocytes with IC50 of 3.1uM, also is a competitive antagonist of nicotinic acid-induced MAPK signaling in cells overexpressing eithermgPR109a or hGPR109a; possesses plasma FFA lowering effects in mice comparable to those of nicotinic acid, does not induce vasodilation. Atherosclerosis Phase 2 Discontinued