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Benfluorex hydrochloride  (Synonyms: JP-992 hydrochloride)

Cat. No.: HY-B1058 Purity: 99.96%
COA Handling Instructions

Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.

For research use only. We do not sell to patients.

Benfluorex hydrochloride Chemical Structure

Benfluorex hydrochloride Chemical Structure

CAS No. : 23642-66-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Benfluorex hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.

IC50 & Target

HNF4α[1]

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[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.

Clinical Trial
Molecular Weight

387.82

Formula

C19H21ClF3NO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(C1=CC(CC(NCCOC(C2=CC=CC=C2)=O)C)=CC=C1)(F)F.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 5.88 mg/mL (15.16 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.96%

References
Kinase Assay
[1]

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].

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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

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
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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Benfluorex hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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