GSK256073

GSK256073 is a potent and selective small molecule agonist of the hydroxy-carboxylic acid receptor 2 (HCAR2), also known as G-protein coupled receptor 109A (GPR109A) or HM74A. It was developed by GSK as a non-flushing alternative to niacin for metabolic disorders. In clinical studies involving subjects with type 2 diabetes mellitus and dyslipidemia, GSK256073 reduced serum glucose and non-esterified fatty acid (NEFA) levels through inhibition of lipolysis. The drug demonstrated insulin-sensitizing effects without causing the flushing commonly associated with niacin therapy. Its primary indications investigated were type 2 diabetes mellitus and hyperlipidemia[1][3][4][5][6].

Other names

8-chloro-3-pentyl-7H-purine-2,6-dione8-chloro-3-pentyl-1H-purine-2,6(3H,7H)-dioneCAS 862892-90-8CAS862892-90-8CAS-862892-90-8