Sigma-Aldrich Glucokinase Activator Ii

Assay

≥98% (HPLC)

Quality Level

100

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 K_Mfor 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%;C _max= 1490 ng/mL;t _1/2= 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 K_Mfor 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: yesPrimary 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.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany