MK-0893

MK-0893 is a potent, selective, reversible, and competitive small molecule antagonist of the glucagon receptor (GCGR), developed by Merck for the treatment of type 2 diabetes mellitus. It binds with high affinity to an allosteric site on the human GCGR (IC50 = 6.6 nM), inhibiting glucagon-induced cAMP production and thereby reducing fasting and postprandial plasma glucose levels. In clinical trials up to Phase 2, once-daily oral dosing led to significant reductions in blood glucose and HbA1c with a low incidence of hypoglycemia. However, development was discontinued due to observed increases in LDL cholesterol, liver transaminases, body weight, and blood pressure in some studies[1][2][3][4][5][6][7].

Other names

(S)-3-(4-(1-(3-(3,5-Dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl)ethyl)benzamido)propanoic acid