851884-87-2
Chemical Structure
GKA50
- CAS No.: 851884-87-2
- Formula:C26H28N2O6
- Molecular Weight:464.51
IUPAC Name: 6-(3-(((S)-1-methoxypropan-2-yl)oxy)-5-(((S)-1-phenylpropan-2-yl)oxy)benzamido)nicotinic acid
InChIKey: OCBMECSFDVUYQN-ROUUACIJSA-N
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
Biological Activity: 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].
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GKA50 | 99.84% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
