Biological Activity
Glucokinase partial activator (EC50 = 174 nM). Acts synergistically with metformin (Cat. No. 2864) to improve glycemic control in adult with type 2 diabetes.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 432.43 |
| Formula | C22H20N6O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1245603-92-2 |
| PubChem ID | 46916694 |
| InChI Key | MASKQITXHVYVFL-UHFFFAOYSA-N |
| Smiles | CC1=CC2=C(OC3=CN=C(C(N(C)C)=O)N=C3)C=C(C(NC4=CN=C(C)C=N4)=O)C=C2O1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.24 | 100 |
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 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 | 2.31 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
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 PMID:
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
Keywords: PF 04937319, supplier, PF04937319, Glucokinase, partial, activators, activates, type, 2, diabetes, Hexokinases, Tocris Bioscience
