ChemicalBook--->CAS DataBase List--->851884-87-2

851884-87-2

851884-87-2 Structure

851884-87-2 Structure
IdentificationBack Directory
[Name]

GKA-50
[CAS]

851884-87-2
[Synonyms]

GKA50
GKA-50
GKA 50
GKA-50; GKA 50
OCBMECSFDVUYQN-ROUUACIJSA-N
6-[[3-[(1S)-2-Methoxy-1-Methylethoxy]-5-[(1S)-1-Methyl-2-phenylethoxy]benzoyl]aMino]-3-pyridinecarboxylic Acid
[Molecular Formula]

C26H28N2O6
[MOL File]

851884-87-2.mol
[Molecular Weight]

464.51
Chemical PropertiesBack Directory
[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
[form ]

powder
[pka]

3.49±0.10(Predicted)
[color ]

white to beige
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H413
[Precautionary statements ]

P273-P301+P312+P330
[Hazard Codes ]

Xn
[Risk Statements ]

22
[WGK Germany ]

3
Hazard InformationBack Directory
[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 cellsGKA50 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, 30?mg/kg
Administration:Oral administration
Result:Significant percentage glucose lowering.
[storage]

Store at -20°C
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