| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Benfluorex targets multiple pathways. It acts as a serotonin and dopamine reuptake inhibitor, blocking the reuptake of these neurotransmitters in the synaptic cleft. It is also a hepatic nuclear factor 4 alpha (HNF4α) activator. It consistently activates insulin promoter activity. It is classified as an orphan receptor ligand.
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| ln Vitro |
Benfluex hydrochloride increases the amount of GFP-positive cells, a sustainable way to stimulate insulin promoter activity. In a dose-dependent manner, benfluex hydrochloride raises endogenous insulin mRNA levels and the quantity of GFP-positive cells. Benfluex hydrochloride increases the expression of HNF4α, which is consistent with its role as an activator of HNF4α. HNF4α protease's sensitivity is altered by benfluex hydrochloride, but not by an inert control drug [1]. In oleic acid, benfluex hydrochloride decreases the synthesis of ketone bodies and acid lysates in a concentration-dependent manner, but it dramatically increases the amount of 14CO2 that enters the citric acid cycle. In a dose-dependent way, benfluex hydrochloride reduces the rate of gluconeogenesis from lactate/pyruvate (10/1 nM) [2].
In vitro, benfluorex hydrochloride consistently activates insulin promoter activity as measured by an increased number of GFP-positive cells. It functions as a serotonin and dopamine reuptake inhibitor. It activates HNF4α, a nuclear receptor involved in the regulation of glucose and lipid metabolism. |
| ln Vivo |
In vivo, benfluorex has been used as an anorectic and hypolipidemic drug. For poorly controlled type 2 diabetes patients, it can improve glycemic control and reduce insulin resistance. It was used for the treatment of obesity and diabetes. Its use has been limited due to safety concerns related to its structural similarity to fenfluramine.
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| Enzyme Assay |
In vitro binding assays for benfluorex typically involve evaluating its affinity for serotonin and dopamine transporters using radioligand binding. Membrane preparations from cells expressing the transporters are incubated with radiolabeled ligands and varying concentrations of the compound. IC50 or Ki values are calculated from displacement curves. HNF4α activation is assessed by reporter gene assays.
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| Cell Assay |
Cell-based assays for benfluorex involve culturing insulin-producing cells or hepatocytes in appropriate media. Cells are treated with benfluorex at concentrations ranging from 0.1 µM to 100 µM for 24-72 hours. Insulin promoter activity is measured by reporter gene assays. Glucose uptake and metabolism are assessed. Neurotransmitter reuptake is measured in neuronal cell lines. Cytotoxicity is assessed by standard viability assays.
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| Animal Protocol |
In vivo animal experiments for benfluorex typically involve administration to rodent models of obesity or diabetes via oral gavage. Body weight and food intake are monitored. Glucose tolerance tests and insulin sensitivity tests are performed. Lipid profiles are measured. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and tissues. Comprehensive toxicology studies have been conducted due to its clinical use.
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| ADME/Pharmacokinetics |
Benfluorex HCl (molecular weight 387.82, formula C19H21ClF3NO2) is orally active. It is metabolized in the liver to its active metabolite, norfenfluramine. It has a long half-life supporting once- or twice-daily dosing. Detailed pharmacokinetic parameters are available in clinical pharmacology literature. Its use has been associated with valvular heart disease.
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| Toxicity/Toxicokinetics |
Benfluorex has been associated with valvular heart disease and pulmonary hypertension due to its structural similarity to fenfluramine and its metabolism to norfenfluramine. These safety concerns have led to its withdrawal from the market in many countries. Comprehensive toxicological evaluation has been conducted. The compound is for research use only.
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| References | |
| Additional Infomation |
Benfluorex HCl (CAS#: 23642-66-2) is an anorectic and hypolipidemic agent. It is a serotonin and dopamine reuptake inhibitor and HNF4α activator. It improves glycemic control in type 2 diabetes. It was withdrawn due to valvular heart disease risk. Molecular weight: 387.82.
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| Molecular Formula |
C19H21CLF3NO2
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| Molecular Weight |
387.82374
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| Exact Mass |
387.121
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| CAS # |
23642-66-2
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| Related CAS # |
Benfluorex;23602-78-0
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| PubChem CID |
198015
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| Appearance |
White to off-white solid powder
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| Density |
1.183g/cm3
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| Boiling Point |
420.5ºC at 760mmHg
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| Melting Point |
158-159?C
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| Flash Point |
208.1ºC
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| Vapour Pressure |
2.81E-07mmHg at 25°C
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| LogP |
5.275
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
408
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NLOALSPYZIIXEO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20F3NO2.ClH/c1-14(12-15-6-5-9-17(13-15)19(20,21)22)23-10-11-25-18(24)16-7-3-2-4-8-16/h2-9,13-14,23H,10-12H2,1H31H
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| Chemical Name |
2-((1-(3-(trifluoromethyl)phenyl)propan-2-yl)amino)ethyl benzoate hydrochloride
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| Synonyms |
Benfluorex hydrochloride Lipophoral Mediator JP 992 EINECS 245-801-8 Mediaxal Balans EINECS 245-020-2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~257.85 mM)
H2O : ~2.27 mg/mL (~5.85 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5.88 mg/mL (15.16 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5785 mL | 12.8926 mL | 25.7852 mL | |
| 5 mM | 0.5157 mL | 2.5785 mL | 5.1570 mL | |
| 10 mM | 0.2579 mL | 1.2893 mL | 2.5785 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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