Benfluorex-hydrochloride-JP-992-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBenfluorex hydrochlorideCat. No.: HY-B1058CAS No.: 23642-66-2Synonyms: JP-992 hydrochloride分式: CHClFNO分量: 387.82作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 310 mg/

2、mL (799.34 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5785 mL 12.8926 mL 25.7852 mL5 mM 0.5157 mL 2.5785 mL 5.1570 mL10 mM 0.2579 mL 1.2893 mL 2.5785 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Benfluorex hydrochloride (JP

3、-992 hydrochloride)个肝核因 4 (HNF4) 激活剂。IC50 & Target HNF4 1体外研究Benfluorex hydrochloride consistently activates insulin promoter activity as measured by an increased1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEnumber of GFP-positive cells. Benfluorex hydrochloride increases the number of GFP-positi

4、ve cells in adose-responsive manner and increases the level of endogenous insulin mRNA. Consistent with being HNF4activator, Benfluorex hydrochloride stimulates HNF4 expression. Benfluorex hydrochloride alters HNF4protease sensitivity, while the inactive control compound does not 1. Benfluorex hydro

5、chloride decreases, ina 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 hydrochloride.Benfluorex hydrochloride inhibits in a dose-dependent manner the rates

6、 of gluconeogenesis fromlactate/pyruvate (10/1 nM) 2.PROTOCOLKinase Assay 1 HepG2 cells are treated with DMSO or Benfluorex hydrochloride at a concentration of 20 M or 40 M for 16hr.Total cell protein is extracted, measured by BCA protein assay. Each sample is split into two aliquots forproteolysis

7、without (-) or with (+) Subtilisin. Twenty ug of cell lysate is incubated with or without protease (20ng/mL subtilisin) for 35 minutes at room temperature. Western blot is then performed with primary anti-HNF4 polyclonal antibody (1:1000 dilution) and secondary HRP conjugated anti-goat IgG (1:2000 d

8、ilution),detected with chemiluminescence ECL kit 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 Hepatocytes are isolated by in situ perfusion of the liver with 0.025% collagenase. Hepatocytes (1 to 2106cells/mL) are incubated at 37C in 2

9、 mL of oxygenated (O2:CO2; 95:5) Krebs-Henseleit bicarbonate buffer(pH 7.4) for 1 h in a gyratory shaking water bath. Benfluorex hydrochloride is dissolved in DMSO and added(10 L) to the incubation medium at a final concentration of 0.1 or 1 nM 2.MCE has not independently confirmed the accuracy of t

10、hese methods. They are for reference only.REFERENCES1. Lee SH, et al. Identification of alverine and benfluorex as HNF4 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 geneexpression. Diabetes. 2002 Aug;51(8):2363-8.McePdfHeightCaution: Product has not been fully v