Background:

Ampkinone is an AMPK activator.

Adenosine 5'-monophosphate (AMP) activated protein kinase (AMPK) has considered as an promising target molecule for the treatment of metabolic disorders, such as obesity and type 2 diabetes.

In vitro: Ampkinone was identified as an indirect AMPK activator, which was derived from the small molecule library constructed by diversity-oriented synthesis. Ampkinone was able to stimulate the phosphorylation of AMPK through the indirect activation of AMPK in various cell lines. Moreover, ampkinone-mediated activation of AMPK needed the activity of LKB1 and led to increased glucose uptake in muscle cells [1].

In vivo: Animal study found that ampkinone-treated DIO mice had significantly reduced total body weight and overall fat mass. Histological examination and measurement of lipid parameters showed that ampkinone could effectively improve metabolic abnormalities. These results demonstrated that ampkinone had a potential as a new class of therapeutic agent for antidiabetic and antiobesity treatment through the indirect stimulation of AMPK [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Oh, S. ,Kim, S.J.,Hwang, J.H., et al. Antidiabetic and antiobesity effects of ampkinone (6f), a novel small molecule activator of AMP-activated protein kinase. Journal of Medicinal Chemistry 53, 7405-7413 (2010).