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BOC Sciences |
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1-631-485-4226; 16314854226 |
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info@bocsci.com |
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| Product Name: | GKA-50 | | Synonyms: | GKA 50;GKA50;GKA-50;6-[[3-[(1S)-2-Methoxy-1-Methylethoxy]-5-[(1S)-1-Methyl-2-phenylethoxy]benzoyl]aMino]-3-pyridinecarboxylic Acid;OCBMECSFDVUYQN-ROUUACIJSA-N;GKA-50; GKA 50;3-Pyridinecarboxylic acid, 6-[[3-[(1S)-2-methoxy-1-methylethoxy]-5-[(1S)-1-methyl-2-phenylethoxy]benzoyl]amino]- | | CAS: | 851884-87-2 | | MF: | C26H28N2O6 | | MW: | 464.51 | | EINECS: | | | Product Categories: | | | Mol File: | 851884-87-2.mol |  |
| | GKA-50 Chemical Properties |
| Boiling point | 607.0±55.0 °C(Predicted) | | density | 1.247±0.06 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | DMSO: soluble15mg/mL, clear | | pka | 3.49±0.10(Predicted) | | form | powder | | color | white to beige | | InChIKey | OCBMECSFDVUYQN-ROUUACIJSA-N | | SMILES | N(c3ncc(cc3)C(=O)O)C(=O)c1cc(cc(c1)O[C@H](Cc2ccccc2)C)O[C@H](COC)C |
| Hazard Codes | Xn | | Risk Statements | 22 | | WGK Germany | 3 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Acute Tox. 4 Oral
Aquatic Chronic 4 |
| | GKA-50 Usage And Synthesis |
| Uses | 6-[[3-[(1S)-2-Methoxy-1-methylethoxy]-5-[(1S)-1-methyl-2-phenylethoxy]benzoyl]amino]-3-pyridinecarboxylic Acid, is one of the glucokinase activator derivatives. GKAs activate GK via binding to an allosteric site of the enzyme. They increase glucose-stimulated insulin secretion and decrease blood glucose levels. Also, glucokinase activator GKA50 is shown to be able to promote proliferation by increasing the cell volume and thus, preventing apoptosis in rat pancreatic insulinoma-1 beta cell. | | Biological Activity | GKA50 is a specific activator of glucokinase (EC50 = 0.03 μM). In mouse MIN6 insulin-secreting cells and r at pancreatic islet cells, GKA50 elicits a leftward shift in response to sub-maximal glucose concentrations as measured by insulin secretion and elevation of intracellular calcium levels. | | in vivo | GKA50 (1-30 mg/kg; p.o.) gives significant glucose lowering in an oral glucose tolerance test[1]. | Animal Model: | High-fat-fed obese female Zucker (fa/fa) rats[1] | | Dosage: | 1, 3, 10, 30mg/kg | | Administration: | Oral administration | | Result: | Significant percentage glucose lowering. |
| | storage | Store at -20°C |
| | GKA-50 Preparation Products And Raw materials |
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