Description
FSG67 (1158383-34-6) is an inhibitor of Glycerol 3-Phosphate Acyltransferase (GPAT); IC50?= 24 μM.1?It was able to reduce food intake, decrease body weight and adiposity, enhance energy utilization as fatty acid oxidation, reverse hepatic steatosis, and enhance insulin sensitivity in diet-induced obese mice while showing no?in vitro?or?in vivo?toxicity.2?FSG67 also caused decreased gene expression for orexigenic hypothalamic neuropeptides AgRP and NPY.2?FSG67 increased FAOx in primary hypothalamic neurons (PHN) leading to an increase in ATP and inactivation of AMPK. Oxidative stress and indicators of ER stress were also reduced in PHN.3
References
1) Wydysh?et al. (2009),?Design and Synthesis of Small Molecule Glycerol 3-Phosphate Acyltransferase Inhibitors; J. Med. Chem.,?52?3317
2) Kuhajda?et al. (2011),?Pharmacological glycerol-3-phosphate acyltransferase inhibition decreases food intake and adiposity and increases insulin sensitivity; Am. J. Physiol. Regul. Integr. Comp. Physiol.,?301?R116
3) McFadden?et al. (2014),?Increasing Fatty Acid Oxidation Remodels the Hypothalamic Neurometabolome to Mitigate Stress and Inflammation; PLoS ONE,?9?e115642