2. Metabolic Enzyme/Protease Autophagy
  3. FXR Autophagy
  4. Fexaramine

Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.

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

Fexaramine Chemical Structure

Fexaramine Chemical Structure

CAS No. : 574013-66-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 145 In-stock
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Solid
1 mg USD 34 In-stock
5 mg USD 85 In-stock
10 mg USD 132 In-stock
50 mg USD 396 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 7 publication(s) in Google Scholar

Fexaramine Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors[1][2].

In Vitro

Bile acid treatment is performed in HuTu-80 cells with Fexaramine (5, 25, and 50 μM) for 24 h. Fexaramine (50 μM) increases small heterodimer partner (SHP) transcript levels by 2.1-fold. The cells are treated with various concentrations of Fexaramine, and the endogenous secretin transcript levels are significantly reduced (33% in 50 μM Fexaramine). Fexaramine treatment also significantly suppresses secretin promoter activity by 32%[1].

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

Fexaramine Related Antibodies
In Vivo

Fexaramine treatment of DIO mice produces a striking metabolic profile that includes reduced weight gain, decreased inflammation, browning of WAT and increased insulin sensitization[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

496.64

Formula

C32H36N2O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CN(C)C1=CC=C(C2=CC=C(CN(C3=CC(/C=C/C(OC)=O)=CC=C3)C(C4CCCCC4)=O)C=C2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (100.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0135 mL 10.0677 mL 20.1353 mL
5 mM 0.4027 mL 2.0135 mL 4.0271 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: 2.75 mg/mL (5.54 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.03 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.
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).
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: 99.24%

COA (246 KB) LCMS (122 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0135 mL 10.0677 mL 20.1353 mL 50.3383 mL
5 mM 0.4027 mL 2.0135 mL 4.0271 mL 10.0677 mL
10 mM 0.2014 mL 1.0068 mL 2.0135 mL 5.0338 mL
15 mM 0.1342 mL 0.6712 mL 1.3424 mL 3.3559 mL
20 mM 0.1007 mL 0.5034 mL 1.0068 mL 2.5169 mL
25 mM 0.0805 mL 0.4027 mL 0.8054 mL 2.0135 mL
30 mM 0.0671 mL 0.3356 mL 0.6712 mL 1.6779 mL
40 mM 0.0503 mL 0.2517 mL 0.5034 mL 1.2585 mL
50 mM 0.0403 mL 0.2014 mL 0.4027 mL 1.0068 mL
60 mM 0.0336 mL 0.1678 mL 0.3356 mL 0.8390 mL
80 mM 0.0252 mL 0.1258 mL 0.2517 mL 0.6292 mL
100 mM 0.0201 mL 0.1007 mL 0.2014 mL 0.5034 mL
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Fexaramine 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.

Keywords:

Fexaramine574013-66-4FXRAutophagyNR1H4Inhibitorinhibitorinhibit

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