AdipoR1 and AdipoR2 agonist, first orally active
CAS：924416-43-3
分子式：C27H28N2O3
分子量：428.52
纯度：98%
存储：Store at -20°C

Background:

AdipoRon is an agonist of AdipoR1 and AdipoR2 with Kd values of 1.8 and 3.1 μM, respectively [1].

Adiponectin receptor (AdipoR) is a receptor for adiponectin, which is a protein and plays an important role in regulating glucose levels and fatty acid breakdown.

AdipoRon is the first orally active AdipoR1 and AdipoR2 agonist. AdipoRon (5-50 μM) increased AMPK phosphorylation via AdipoR1 in a dose-dependent way. Also, AdipoRon replenished adiponectin-stimulated AMPK phosphorylation. In C2C12 myotubes, AdipoRon increased PGC-1α expression and mitochondrial DNA content in a Ca2+- and dose-dependent way [1].

In wild-type mice, AdipoRon (50mg/kg) significantly induced AMPK phosphorylation in liver and skeletal muscle. Also, AdipoRon (50mg/kg) significantly reduced fasting plasma insulin and glucose levels. In wild-type mice fed a high-fat diet, AdipoRon increased the expression levels of

PPAR-α via AdipoR2 and reduced plasma levels of free fatty acid (FFA) and triglycerides. Also, AdipoRon reduced the expression levels of pro-inflammatory cytokines such as TNF-α and MCP-1 in the liver. In db/db obese mice, AdipoRon significantly reduced plasma glucose levels and ameliorated insulin resistance, glucose intolerance and dyslipidaemia [1]. In wild type mice, AdipoRon significantly improved cardiac function and inhibited myocardial ischemia/reperfusion (MI/R)-induced apoptosis [2].

参考文献:
[1].  Okada-Iwabu M, Yamauchi T, Iwabu M, et al. A small-molecule AdipoR agonist for type 2 diabetes and short life in obesity. Nature, 2013, 503(7477): 493-499.
[2].  Zhang Y, Zhao J, Li R, et al. AdipoRon, the First Orally Active Adiponectin Receptor Activator, Attenuates Post-Ischemic Myocardial Apoptosis. Am J Physiol Endocrinol Metab, 2015, ajpendo.00577.2014.