Benfluorex hydrochloride
Based on 5 publication(s) in Google Scholar
Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.
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- Reinheit: 99.96%
- CAS. Nr.: 23642-66-2
- Formel: C19H21ClF3NO2
- Molecular Weight:387.82
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Benfluorex hydrochloride
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RT-PCR
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biologische Aktivität
HNF4α[1]
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[1]. 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)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 23642-66-2
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Appearance Solid
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Molecular Weight 387.82
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Formel C19H21ClF3NO2
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Color White to off-white
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SMILES
FC(C1=CC(CC(NCCOC(C2=CC=CC=C2)=O)C)=CC=C1)(F)F.[H]Cl
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Synonyms
JP-992 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Short-Term Statin Therapy Induces Hepatic Insulin Resistance Through HNF4α/PAQR9/PPM1α Axis Regulated AKT Phosphorylation. [Abstract]2024 Sep;11(34):e2403451. PMID: 38970167
Benfluorex hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Sep;11(34):e2403451. [Abstract]
Relative mRNA levels of Paqr9, Ulk1, Cyp7a1 and Lipc in mouse primary hepatocytes with atorvastatin (Ator) and different concentration of Benfluorex hydrochloride (BFX) (2-50 μM).
Benfluorex hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Sep;11(34):e2403451. [Abstract]
Benfluorex hydrochloride (B) (20 mg/kg; i.g.; every other day for 3 weeks) improved levels of fasting glucose affected by atorvastatin treatment in Paqr9-/- mice.
Benfluorex hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Sep;11(34):e2403451. [Abstract]
Benfluorex hydrochloride (B) (20 mg/kg; i.g.; every other day for 3 weeks) improved levels of insulin and FFA affected by atorvastatin treatment in Paqr9-/- mice.
Benfluorex hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Sep;11(34):e2403451. [Abstract]
Benfluorex hydrochloride (B) (20 mg/kg; i.g.; every other day for 3 weeks) increased hepatic AKT1 phosphorylation and lowered the PAQR9 levels raised by atorvastatin in Paqr9-/- mice.
Benfluorex hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Sep;11(34):e2403451. [Abstract]
Benfluorex hydrochloride (B) (20 mg/kg; i.g.; every other day for 3 weeks) alleviated glucose tolerance and insulin tolerance of Paqr9-/- mice.
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EBioMedicine
Intestinal epithelial β Klotho is a critical protective factor in alcohol-induced intestinal barrier dysfunction and liver injury. [Abstract]2022 Aug:82:104181. PMID: 35908416 -
Biochem Pharmacol
AMPKα2/HNF4A/BORIS/GLUT4 pathway promotes hepatocellular carcinoma cell invasion and metastasis in low glucose microenviroment. [Abstract]2022 Sep:203:115198. PMID: 35940258 -
Virol J
GATA binding protein 4 promotes the expression and transcription of hepatitis B virus by facilitating hepatocyte nuclear factor 4 alpha in vitro. [Abstract]2021 Sep 28;18(1):196. PMID: 34583732 -
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (257.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2.27 mg/mL (5.85 mM; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
HepG2 cells are treated with DMSO or Benfluorex hydrochloride at a concentration of 20 µM or 40 µM for 16 hr.Total cell protein is extracted, measured by BCA protein assay. Each sample is split into two aliquots for proteolysis without (-) or with (+) Subtilisin. Twenty ug of cell lysate is incubated with or without protease (20 ng/mL subtilisin) for 35 minutes at room temperature. Western blot is then performed with primary anti-HNF4α polyclonal antibody (1:1000 dilution) and secondary HRP conjugated anti-goat IgG (1:2000 dilution), detected with chemiluminescence ECL kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Hepatocytes are isolated by in situ perfusion of the liver with 0.025% collagenase. Hepatocytes (1 to 2×106 cells/mL) are incubated at 37°C in 2 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 μL) to the incubation medium at a final concentration of 0.1 or 1 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (394 KB)
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- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Lee SH, et al. Identification of alverine and benfluorex as HNF4α activators. ACS Chem Biol. 2013 Aug 16;8(8):1730-6. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.5785 mL | 12.8926 mL | 25.7852 mL | 64.4629 mL |
| 5 mM | 0.5157 mL | 2.5785 mL | 5.1570 mL | 12.8926 mL | |
| DMSO | 10 mM | 0.2579 mL | 1.2893 mL | 2.5785 mL | 6.4463 mL |
| 15 mM | 0.1719 mL | 0.8595 mL | 1.7190 mL | 4.2975 mL | |
| 20 mM | 0.1289 mL | 0.6446 mL | 1.2893 mL | 3.2231 mL | |
| 25 mM | 0.1031 mL | 0.5157 mL | 1.0314 mL | 2.5785 mL | |
| 30 mM | 0.0860 mL | 0.4298 mL | 0.8595 mL | 2.1488 mL | |
| 40 mM | 0.0645 mL | 0.3223 mL | 0.6446 mL | 1.6116 mL | |
| 50 mM | 0.0516 mL | 0.2579 mL | 0.5157 mL | 1.2893 mL | |
| 60 mM | 0.0430 mL | 0.2149 mL | 0.4298 mL | 1.0744 mL | |
| 80 mM | 0.0322 mL | 0.1612 mL | 0.3223 mL | 0.8058 mL | |
| 100 mM | 0.0258 mL | 0.1289 mL | 0.2579 mL | 0.6446 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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