AM-2394 _Glucokinase Activator - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAM-2394Cat. No.: HY-100221CAS No.: 1442684-77-6分式: CHNO分量: 423.47作靶点: Glucokinase作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 30 mg/mL (70.84 mM)* means sol

2、uble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3614 mL 11.8072 mL 23.6144 mL5 mM 0.4723 mL 2.3614 mL 4.7229 mL10 mM 0.2361 mL 1.1807 mL 2.3614 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 AM-2394种新型的 glucokinase 激活剂 (GKA)。AM-2394激活葡萄糖激酶 (GK)

3、，EC50 为 60 nM。IC50 & Target EC50: 60 nM (glucokinase) 1体内研究AM-2394, a structurally distinct glucokinase activator that displays a robust reduction in plasma glucoseduring an oral glucose tolerance test (OGTT) in ob/ob mice at a dose of 3 mg/kg. AM-2394 increases the1/2 Master of Small Molecules 您边的抑

4、制剂师www.MedChemEaffinity of glucokinase (GK) for glucose by approximately 10-fold, exhibits moderate clearance and good oralbioavailability in multiple animal models, and lowers glucose excursion following an oral glucose tolerancetest in an ob/ob mouse model of diabetes. AM-2394 exhibits good-to-mod

5、erate cross species plasmaclearance, volume of distribution, and oral bioavailability, allowing for further evaluation in animal models 1.PROTOCOLAnimal Mice 1Administration 1 In order to determine the effect of AM-2394 in an animal model of type 2 diabetes, it was administered per os(PO) to male ob

6、/ob mice 30 minutes prior to performing an oral glucose tolerance test (OGTT). Doses of 1, 3,10, 30 mg/kg each reduced glucose excursion, with maximal efficacy seen at 3 mg/kg.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Dransfield PJ, et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med Chem Lett. 2016May 23;7(7):714-8.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.