Delving into the Latest Updates on AM-2394 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

AM-2394

Target

glucokinase

Action

activators

Mechanism

glucokinase activators(Glucokinase activators)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication-

Inactive Indication

Diabetes Mellitus, Type 2

Originator Organization

Amgen, Inc.

Array BioPharma, Inc.

Active Organization-

Inactive Organization

Array BioPharma, Inc.

Amgen, Inc.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC22H25N5O4

InChIKeyQUISANLDBDCMPD-UHFFFAOYSA-N

CAS Registry1442684-77-6

Author: Lai, Sujen ; DeWolf, Walter E. ; Veniant-Ellison, Murielle ; Cheng, Alan ; Xiong, Yumei ; Kraser, Christopher F. ; Houze, Jonathan ; Coward, Peter ; Condroski, Kevin R. ; Medina, Julio C. ; Pattaropong, Vatee ; Tien, Eric ; Fu, Zice ; Boyd, Steven A. ; Du, Xiaohui ; Conn, Marion ; Kohn, Todd J. ; Hinklin, Ronald J. ; Komorowski, Renee ; Voegtli, Walter C. ; Jin, Lixia ; Aicher, Thomas D. ; Dransfield, Paul J.

Glucokinase (GK) catalyzes the phosphorylation of glucose to glucose-6-phosphate. We present the structure-activity relationships leading to the discovery of AM-2394, a structurally distinct GKA. AM-2394 activates GK with an EC50 of 60 nM, increases the affinity of 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.

14 Jul 2016·ACS medicinal chemistry lettersQ3 · MEDICINE

5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties

Q3 · MEDICINE

Article

Author: Jin, Lixia ; DeWolf, Walter E. ; Houze, Jonathan ; Medina, Julio C. ; Jiao, Xianyun ; Pattaropong, Vatee ; Conn, Marion ; Fu, Zice ; Lai, SuJen ; Du, Xiaohui ; Coward, Peter ; Kohn, Todd J. ; Kraser, Christopher F. ; Cardozo, Mario ; Chow, David ; Hinklin, Ronald J. ; Xiong, YuMei ; Dransfield, Paul ; Veniant, Murielle ; Boys, Mark L. ; Komorowski, Renee

Two 1-(4-aryl-5-alkyl-pyridin-2-yl)-3-methylurea glucokinase activators were identified with robust in vivo efficacy. These two compounds possessed higher solubilities than the previously identified triaryl compounds (i.e., AM-2394). Structure-activity relationship studies are presented along with relevant pharmacokinetic and in vivo data.

100 Deals associated with AM-2394

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Preclinical	United States	Array BioPharma, Inc.	25 May 2016
Diabetes Mellitus, Type 2	Preclinical	United States	Amgen, Inc.	25 May 2016