A glucokinase activator
PF-04937319 is an activator of glucokinase (EC50s = 174, 407, and 269 nM for the recombinant human, rat, and dog enzymes, respectively).1 It increases glucose-induced insulin secretion in isolated rat islets when used at concentrations of 4 and 12 µM.2 PF-04937319 (3-100 mg/kg) reduces postprandial plasma glucose levels in rats.
1.Petterson, J.C., Litchfield, J., Neef, N., et al.The relationship of glucokinase activator-induced hypoglycemia with arteriopathy, neuronal necrosis, and peripheral neuropathy in nonclinical studiesToxicol. Pathol.42(4)696-708(2014) 2.Pffefferkorn, J.A., Guzman-Perez, A., Oates, P.J., et al.Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitusMedchemcomm.2828-839(2011)
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