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Glucokinase partial activator (EC50 = 174 nM). Enhances glucose-stimulated insulin secretion in islet cell cultures and translocation of glucokinase from the nucleus to the cytoplasm in hepatocytes in vitro. Reduces post-prandial plasma glucose levels in an oral glucose tolerance test in rats.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 432.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.31 mL||11.56 mL||23.13 mL|
|5 mM||0.46 mL||2.31 mL||4.63 mL|
|10 mM||0.23 mL||1.16 mL||2.31 mL|
|50 mM||0.05 mL||0.23 mL||0.46 mL|
References are publications that support the biological activity of the product.
Pfefferkorn et al (2011) 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 di Med.Chem.Commun., 2 828
Pettersen et al (2014) The relationship of glucokinase activator-induced hypoglycemia with arteriopathy, neuronal necrosis, and peripheral neuropathy in nonclinical studies. Toxicol. Pathol. 42 696 PMID: 24771080
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