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AMG-1694

Names

[ CAS No. ]:
1361217-07-3

[ Name ]:
AMG-1694

Biological Activity

[Description]:

AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Glucokinase
Research Areas >> Metabolic Disease

[Target]

IC50: 7 nM (GK-GKRP)[1]


[In Vitro]

AMG-1694 is highly effective in restoring the enzymatic activity of GK with an EC50 of 0.020 μM in the presence of GKRP[1].

[References]

[1]. Lloyd DJ, et al. Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors. Nature. 2013 Dec 19;504(7480):437-40.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H30F3N3O4S2

[ Molecular Weight ]:
533.63

Related Compounds