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

Tropifexor (LJN452) is a highly potent agonist of FXR with an EC50 of 0.2 nM.

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

Tropifexor Chemical Structure

Tropifexor Chemical Structure

CAS No. : 1383816-29-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 277 In-stock
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10 mM * 1 mL in DMSO USD 277 In-stock
Solid
1 mg USD 110 In-stock
5 mg USD 209 In-stock
10 mg USD 319 In-stock
50 mg USD 869 In-stock
100 mg USD 1375 In-stock
200 mg USD 2035 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Tropifexor Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Tropifexor (LJN452) is a highly potent agonist of FXR with an EC50 of 0.2 nM[1].

IC50 & Target

EC50: 0.2 nM (FXR)
In Vitro

Tropifexor (compound 1) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM. Robust induction of both BSEP and SHP genes is observed in primary cells by Tropifexor in a concentration-dependent manner.
BSEP induction above vehicle (DMSO) control is observed at concentrations as low as 1 nM, while strong induction of SHP (15-fold above vehicle) is observed at 10 nM and modest induction of SHP at 1 nM (3-fold)[1].

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

Tropifexor Related Antibodies
In Vivo

Tropifexor (compound 1) demonstrates highly potent induction of SHP and FGF15 in the ileum as doses as low as 0.1 mg/kg. In the liver, robust induction of SHP is observed at 0.01 mg/kg of Tropifexor with maximal levels of gene induction achieved at 0.3 mg/kg. Expression of CYP8B1 mRNA following 14 day treatment with Tropifexor is already apparent at the lowest dose (0.003 mg/kg), and CYP8B1 gene expression is fully repressed at doses above 0.03 mg/kg.
Treatment of rats with Tropifexor exhibits a clear dose-dependent increase in plasma FGF15 protein, with maximal levels of FGF15 detected at 7 h postdose.
Treatment with Tropifexor for 14 days produces a robust dose-dependent reduction in serum triglycerides and reaches a maximal response with a 0.3 mg/kg dose, resulting in a decrease of triglyceride levels to approximately 79% below the vehicle control group[1].

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

603.58

Formula

C29H25F4N3O5S
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

FC(F)(F)OC(C=CC=C1)=C1C2=NOC(C3CC3)=C2CO[C@@H]4C[C@H]5N(C6=NC7=C(F)C=C(C(O)=O)C=C7S6)[C@H](CC5)C4
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 : ≥ 80.66 mg/mL (133.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6568 mL 8.2839 mL 16.5678 mL
5 mM 0.3314 mL 1.6568 mL 3.3136 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)

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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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.14 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

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(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: 99.35%

COA (252 KB) LCMS (113 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Primary rat hepatocytes are plated in 24 well plates and incubated with a 5 point dose response of Tropifexor (compound 1) for 24 hours. RNA is harvested from the cells using the RNeasy 96 kit. Quantitative PCR is performed. The fold change of the transcript over no stimulation is calculated using the ΔΔCt method, with DMSO (vehicle control) being no stimulation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Adult male wild-type Sprague-Dawley rats are used in this study. All animals are fasted for 3 hours before oral dosing with Tropifexor (compound 1) or with vehicle. Tropifexor is administered orally using a range of four doses (0.03, 0.1, 0.3, and 1.0 mg/kg) and compare directly to the vehicle control group (vehicle: 0.5% methylcellulose, 0.5% Tween 80, 99% water, suspension). Animals are sacrificed seven hours after dosing using CO2, liver, ileum and whole blood (in heparinized tubes) samples are collected for analysis[1].

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, 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 1.6568 mL 8.2839 mL 16.5678 mL 41.4195 mL
5 mM 0.3314 mL 1.6568 mL 3.3136 mL 8.2839 mL
10 mM 0.1657 mL 0.8284 mL 1.6568 mL 4.1420 mL
15 mM 0.1105 mL 0.5523 mL 1.1045 mL 2.7613 mL
20 mM 0.0828 mL 0.4142 mL 0.8284 mL 2.0710 mL
25 mM 0.0663 mL 0.3314 mL 0.6627 mL 1.6568 mL
30 mM 0.0552 mL 0.2761 mL 0.5523 mL 1.3807 mL
40 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0355 mL
50 mM 0.0331 mL 0.1657 mL 0.3314 mL 0.8284 mL
60 mM 0.0276 mL 0.1381 mL 0.2761 mL 0.6903 mL
80 mM 0.0207 mL 0.1035 mL 0.2071 mL 0.5177 mL
100 mM 0.0166 mL 0.0828 mL 0.1657 mL 0.4142 mL
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Tropifexor 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:

Tropifexor1383816-29-2LJN452LJN 452LJN-452FXRAutophagyNR1H4Inhibitorinhibitorinhibit

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