Benfluorex hydrochloride

SKU: orb1225561

Description

Benfluorex is an anorectic and hypolipidemic agent that is structurally related to fenfluramine. It was patented and manufactured by a French pharmaceutical company Servier. On 18 December 2009, the European Medicines Agency (EMEA) recommended the withdrawal of all medicines containing benfluorex in the European Union, because their risks, particularly the risk of heart valve disease (fenfluramine-like cardiovascular side-effects), are greater than their benefits.(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 14CO2 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).

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 23642-66-2
• MW: 387.82
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₁ClF₃NO₂
• SMILES: O=C(OCCNC(C)CC1=CC=CC(C(F)(F)F)=C1)C2=CC=CC=C2.[H]Cl
• Target: HNF4α
• Solubility: Soluble in DMSO

Bioactivity

• 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 14CO2 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Benfluorex HCl | Benfluorex hydrochloride | Lipophoral | Mediator | JP 992

Quick Database Links

Gene Symbol

HNF4α