Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.
性状
Solid
IC50 & Target[1][2]
HNF4α
体外研究(In Vitro)
Benfluorex hydrochloride consistently activates insulin promoter activity as measured by an increased number of GFP-positive cells. Benfluorex hydrochloride 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 hydrochloride stimulates HNF4α expression. Benfluorex hydrochloride alters HNF4α protease sensitivity, while the inactive control compound does not. Benfluorex hydrochloride decreases, in a concentration-dependent manner, the synthesis of acid-soluble products and ketone bodies from oleate, whereas the production of CO2 into citric acid cycle is markedly increased by Benfluorex hydrochloride. Benfluorex hydrochloride inhibits in a dose-dependent manner the rates of gluconeogenesis from lactate/pyruvate (10/1 nM).
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Lee SH, et al. Identification of alverine and benfluorex as HNF4α activators. ACS Chem Biol. 2013 Aug 16;8(8):1730-6.[2]. Kohl C, et al. Effects of benfluorex on fatty acid and glucose metabolism in isolated rat hepatocytes: from metabolic fluxes to gene expression. Diabetes. 2002 Aug;51(8):2363-8.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (257.85 mM)H2O : 2.27 mg/mL (5.85 mM; ultrasonic and warming and heat to 60°C)
[1]. Lee SH, et al. Identification of alverine and benfluorex as HNF4α activators. ACS Chem Biol. 2013 Aug 16;8(8):1730-6.[2]. Kohl C, et al. Effects of benfluorex on fatty acid and glucose metabolism in isolated rat hepatocytes: from metabolic fluxes to gene expression. Diabetes. 2002 Aug;51(8):2363-8.