GKA50

GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose) . GKA50 stimulates insulin release from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca2+-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats[1][2][3][4].

Product Specifications

CAS Number

[851884-87-2]

UNSPSC

12352005

Hazard Statement

H302, H413

Target

Glucokinase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/gka50.html

Concentration

10mM

Purity

99.84

Solubility

DMSO : 46 mg/mL (ultrasonic; warming)

Smiles

O=C(C1=CC=C(NC(C2=CC(O[C@@H](C)CC3=CC=CC=C3)=CC(O[C@@H](C)COC)=C2)=O)N=C1)O

Molecular Formula

C26H28N2O6

Molecular Weight

464.51

Precautions

H302, H413

References & Citations

[1]Coope GJ, et al. Predictive blood glucose lowering efficacy by Glucokinase activators in high fat fed female Zucker rats. Br J Pharmacol. 2006 Oct;149 (3) :328-35.|[2]McGlasson L, et al. The glucokinase activator GKA50 causes an increase in cell volume and activation of volume-regulated anion channels in rat pancreatic β-cells. Mol Cell Endocrinol. 2011 Aug 6;342 (1-2) :48-53.|[3]Johnson D, et al. Glucose-dependent modulation of insulin secretion and intracellular calcium ions by GKA50, a glucokinase activator. Diabetes. 2007;56 (6) :1694-1702.