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Chemical Structure : GKA23
Catalog No.: PC-49828Not For Human Use, Lab Use Only.
GKA23 is a potent, small molecule glucokinase (GK) activator with EC50 of 152 nM for glucokinase activation in 5 mM glucose, increases glucose uptake in primary rat hepatocytes with EC50 of 201 nM.
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GKA23 is a potent, small molecule glucokinase (GK) activator with EC50 of 152 nM for glucokinase activation in 5 mM glucose, increases glucose uptake in primary rat hepatocytes with EC50 of 201 nM.
GKA23 increases the affinity of rat and mouse glucokinase for glucose in vitro.
In biochemical assays using recombinant rat glucokinase, GKA23 increased the affinity of the enzyme for glucose by 18-fold (S 0.5 = 0.54±0.05 mM vs 9.59±0.19 mM in the absence of activator).
GKA23 improved glucose homeostasis in rats by enhancing beta cell insulin secretion and suppressing hepatic glucose production, glucose homeostasis and lipid profile in mice fed a high-fat diet.
| M.Wt | 468.55 | |
| Formula | C21H20N6O3S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Lu M, et al. PLoS One. 2014 Feb 12;9(2):e88431.
2. Baker DJ, et al. Br J Pharmacol. 2014 Apr;171(7):1629-41.
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