1442684-77-6

1442684-77-6 structure

Name: AM 2394
Chemical Name: am2394
CAS Number: 1442684-77-6
Molecular Formula: C₂₂H₂₅N₅O₄
Molecular Weight: 423.47
Catalog: Signaling Pathways Metabolic Enzyme/Protease Glucokinase
Create Date: 2018-04-18 11:36:06
Modify Date: 2024-01-17 06:41:34
AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.

Name	am2394
Synonyms	AM-2394

Description	AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Glucokinase Research Areas >> Metabolic Disease
Target	EC50: 60 nM (glucokinase)[1]
In Vivo	AM-2394, a structurally distinct glucokinase activator that displays a robust reduction in plasma glucose during an oral glucose tolerance test (OGTT) in ob/ob mice at a dose of 3 mg/kg. AM-2394 increases the affinity of glucokinase (GK) for glucose by approximately 10-fold, exhibits moderate clearance and good oral bioavailability in multiple animal models, and lowers glucose excursion following an oral glucose tolerance test in an ob/ob mouse model of diabetes. AM-2394 exhibits good-to-moderate cross species plasma clearance, volume of distribution, and oral bioavailability, allowing for further evaluation in animal models[1].
Animal Admin	Mice[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/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.
References	[1]. Dransfield PJ, et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med Chem Lett. 2016 May 23;7(7):714-8.