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Biological Activity:

AdipoRon is a novel, highly potent, selective and orally active small molecule agonist of adiponectin receptor (AdipoR). AdipoRon binds to both AdipoR1 and AdipoR2 (EC₅₀ for AdipoR1 ~1.8 µM and AdipoR2 ~3.1 µM). AdipoRon showed very similar effects to adiponectin in muscle and liver, such as activation of AMPK and PPAR-α pathways, and ameliorated insulin resistance and glucose intolerance in mice fed with a high-fat diet, which was completely obliterated in AdipoR1 and AdipoR2 double-knockout mice. Moreover, AdipoRon ameliorated diabetes of genetically obese rodent model db/db mice, and prolonged the shortened lifespan of db/db mice on a high-fat diet. AdipoRon could serve as a very useful chemical probe for studies of obesity-related diseases such as type 2 diabetes by activating AdipoR1 and AdipoR2. 

How to Use:

In vitro:  AdipoRon was used at 10-25 µM final concentration in vitro and in cellular assays.

In vivo:  AdipoRon was administered orally to mice at 50 mg/kg once per day. 

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