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5.00487

Sigma-Aldrich

Glucokinase Activator II

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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
Empirical Formula (Hill Notation):
C24H22FN7O3
Molecular Weight:
475.47

assay

≥98% (HPLC)

Quality Level

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

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550602MABS1190MABN702
vibrant-m

5.00487

Glucokinase Activator II

vibrant-m

550602

PKM2 Activator II, DASA

vibrant-m

MABN702

Anti-HK2 Antibody, clone 3D3

assay

≥98% (HPLC)

assay

≥99% (HPLC)

assay

-

assay

-

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

-

manufacturer/tradename

-

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

-

storage condition

-

color

off-white

color

white

color

-

color

-

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.
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 exhibit blood glucose lowering efficacy in OGTT (2 g/kg oral glucose challenge 1 h after single drug oral dosage) test among fasted rats (22% reduction of AUC; 250 mg/kg p.o.) in vivo.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Glucokinase

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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