5.00487
Glucokinase Activator II
Synonym(s):
Glucokinase Activator II, 4-((6-(azetidine-1-carbonyl)-5-fluoropyridin-3-yl)oxy)-2-ethyl-N-(5-methylpyrazin-2-yl)-2H-indazole-6-carboxamide, Hexokinase IV Activator II, Hexokinase D Activator II, GK Activator II
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About This Item
Empirical Formula (Hill Notation):
C24H22FN7O3
CAS Number:
Molecular Weight:
475.47
NACRES:
NA.77
UNSPSC Code:
12352202
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
form
solid
potency
12 nM EC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
General description
A cell-permeable compound that reduces glucokinase Km for glucose (EC₅₀ = 120 nM & 350 nM, for human and rat enzyme). Enhances insulin secretion from INS-1 cells upon glucose exposure.
A cell-permeable indazole derivative that reduces glucokinase Km for glucose (EC50 = 120 nM and 350 nM, respectively, for human and rat enzyme) and effectively enhances insulin secretion from rat insulinima INS-1 cells upon 5 mM glucose exposure (EC50 = 170 nM). Shown to be orally available in rats (F = 69%; Cmax = 1490 ng/mL; t1/2 = 2.6 hr; AUC = 5440 ng·hr/mL; 5 mg/kg p.o.) and exhibit blood glucose lowering efficacy in OGTT (2 g/kg oral glucose challenge 1 h after single drug oral dosage) test on fasted rats (22% reduction of AUC; 250 mg/kg p.o.) in vivo.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Glucokinase
Glucokinase
Preparation Note
Following reconstitution, aliquot and freeze (=2-°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Pfefferkorn, J. A., et al. 2012. Bioorg. Med. Chem. Lett.22, 7100.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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