| Size | Price | |
|---|---|---|
| Other Sizes |
Purity: ≥98%
Benfluorex (Mediator) is an anorectic and hypolipidemic agent that is structurally related to fenfluramine. It may improve glycemic control and decrease insulin resistance in people with poorly controlled type-2 diabetes.
| ln Vitro |
Benfluex regularly increases the amount of GFP-positive cells, a marker of insulin promoter activity. In a dose-dependent manner, benfluex raises endogenous insulin mRNA levels and the number of GFP-positive cells. In line with its role as an HNF4α activator, Benfluex induces the expression of HNF4α. HNF4α protease sensitivity is changed by benfluex, but not by inactive control molecules [1]. Benfluex greatly increases the generation of 14CO2 in the citric acid cycle while decreasing the synthesis of ketone bodies and acid-soluble metabolites in oleic acid in a concentration-dependent way. Benfluex reduces lactate/pyruvate (10/1 nM) gluconeogenesis rate in a dose-dependent manner [2].
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| References |
[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 |
| Additional Infomation |
Benzoic acid 2-[1-[3-(trifluoromethyl)phenyl]propan-2-ylamino]ethyl ester is a benzoate ester.
Benfluorex is an anorectic and hypolipidemic agent that is structurally related to fenfluramine. It was patented and manufactured by a French pharmaceutical company Servier. The European Medicines Agency (EMA) recommended withdrawing all benfluorex containing medicines on 18 December 2009. This recommendation was based on the risks (especially fenfluramine-like cardiovascular side-effects) outweighing the benefits. Benfluorex is an antilipidemic agent that decreases the relative rate of hepatic triacylglycerol synthesis. Benfluorex was never approved for use in the United States and was withdrawn in the European Union because of an increased risk of pulmonary hypertension and valvular disease. See also: Benfluorex hydrochloride (annotation moved to). |
| Molecular Formula |
C19H20F3NO2
|
|---|---|
| Molecular Weight |
386.8158
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| Exact Mass |
387.121
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| CAS # |
23602-78-0
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| Related CAS # |
Benfluorex hydrochloride;23642-66-2
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| PubChem CID |
2318
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.183g/cm3
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| Boiling Point |
420.5ºC at 760 mmHg
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| Flash Point |
208.1ºC
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| Vapour Pressure |
2.81E-07mmHg at 25°C
|
| Index of Refraction |
1.515
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| LogP |
5.275
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
25
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| Complexity |
408
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(CC1=CC(=CC=C1)C(F)(F)F)NCCOC(=O)C2=CC=CC=C2
|
| InChi Key |
CJAVTWRYCDNHSM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20F3NO2/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,10-12H2,1H3
|
| Chemical Name |
2-((1-(3-(trifluoromethyl)phenyl)propan-2-yl)amino)ethyl benzoate
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| Synonyms |
BRN 4152887 JP 992 SE 780 Minolip Mediator EINECS 245-777-9 Benfluramate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5852 mL | 12.9259 mL | 25.8518 mL | |
| 5 mM | 0.5170 mL | 2.5852 mL | 5.1704 mL | |
| 10 mM | 0.2585 mL | 1.2926 mL | 2.5852 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00544518 | UNKNOWN STATUS | Drug: metformin Drug: benfluorex |
Type 2 Diabetes | Air Force Military Medical University, China | 2007-10 | Phase 2 |
| NCT02008552 | COMPLETED | Genetic: Sampling of blood | Blood Sample | University Hospital, Brest | 2013-10-18 | Not Applicable |
| NCT06107322 | RECRUITING | Neutropenia | University Hospital, Strasbourg, France | 2023-03-01 |
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