Potent hepatoselective glucokinase activator (EC50 = 90 nM). Exhibits >50-fold liver to pancreas ratio of tissue distribution. Reduces fasting and postprandial glucose levels with no hypoglycemia in a rat diabetes model.
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.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 396.36. Batch specific molecular weights may vary from batch to batch due to solvent 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||2.52 mL||12.61 mL||25.23 mL|
|5 mM||0.5 mL||2.52 mL||5.05 mL|
|10 mM||0.25 mL||1.26 mL||2.52 mL|
|50 mM||0.05 mL||0.25 mL||0.5 mL|
References are publications that support the biological activity of the product.
Pfefferkorn et al (2012) Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J.Med.Chem. 55 1318 PMID: 22196621
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Keywords: PF 04991532, PF 04991532 supplier, PF04991532, glucokinase, activators, activates, potent, antidiabetic, Hexokinases, Enzyme, Substrates, /, Activators, 6345, Tocris Bioscience
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