Benfluorex

Benfluorex (JP-992) is a hepatic nuclear factor 4 alpha (HNF4α) activator. IC50 & Target: HNF4α^[1] In Vitro: Benfluorex consistently activates insulin promoter activity as measured by an increased number of GFP-positive cells. Benfluorex increases the number of GFP-positive cells in a dose-responsive manner and increases the level of endogenous insulin mRNA. Consistent with being HNF4α activator, Benfluorex stimulates HNF4α expression. Benfluorex alters HNF4α protease sensitivity, while the inactive control compound does not^[1]. Benfluorex decreases, in a concentration-dependent manner, the synthesis of acid-soluble products and ketone bodies from oleate, whereas the production of ¹⁴CO₂ into citric acid cycle is markedly increased by Benfluorex. Benfluorex inhibits in a dose-dependent manner the rates of gluconeogenesis from lactate/pyruvate (10/1 nM)^[2].