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/Citations:

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