GKA23 | Glucokinase activator | Probechem Biochemicals

Chemical Structure : GKA23

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GKA23 (GKA-23)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	468.55
分子式	C21H20N6O3S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(1S)-1-[5-[[3-[(2,6-Dimethyl-3-pyridinyl)oxy]-5-(2-pyridinylthio)-2-pyridinyl]amino]-1,2,4-thiadiazol-3-yl]-1,2-ethanediol

参考文献

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.

GKA23 (GKA-23)

生物&药学活性

物理化学性质&存储条件

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GKA23 (GKA-23)

生物&药学活性

物理化学性质&存储条件

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