Tropifexor
Based on 7 publication(s) in Google Scholar
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.
- Purity: 99.35%
- CAS No.: 1383816-29-2
- Formula: C29H25F4N3O5S
- Molecular Weight:603.58
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tropifexor
More- Science. 2023 Jun 9;380(6649):eabo2296. [Abstract]
- Acta Pharm Sin B. 2023 Feb;13(2):559-576. [Abstract]
- Cancer Lett. 2026 Aug 28:654:218589. [Abstract]
- J Pharm Anal. 2021 Feb;11(1):122-127. [Abstract]
- Biomed Pharmacother. 2024 Apr:173:116331. [Abstract]
- J Biol Chem. 2024 Sep 12:107765. [Abstract]
- bioRxiv. 2024 Feb 8:2023.11.20.567833. [Abstract]
Biological Activity
EC50: 0.2 nM (FXR)
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.
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 No. 1383816-29-2
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Appearance Solid
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Molecular Weight 603.58
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Formula C29H25F4N3O5S
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Color Off-white to yellow
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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
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Synonyms
LJN452
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Science
A microbiota-modulated checkpoint directs immunosuppressive intestinal T cells into cancers. [Abstract]2023 Jun 9;380(6649):eabo2296. PMID: 37289890 -
Acta Pharm Sin B
SIRT1 activation synergizes with FXR agonism in hepatoprotection via governing nucleocytoplasmic shuttling and degradation of FXR. [Abstract]2023 Feb;13(2):559-576. PMID: 36873184 -
Cancer Lett
Bile acid retention impairs tumoral antigen presentation and intrinsic tumor suppression in MASH-HCC. [Abstract]2026 Aug 28:654:218589. PMID: 42173274 -
J Pharm Anal
2021 Feb;11(1):122-127. PMID: 33717618 -
Biomed Pharmacother
Improvement of NASH and liver fibrosis through modulation of the gut-liver axis by a novel intestinal FXR agonist. [Abstract]2024 Apr:173:116331. PMID: 38428307 -
J Biol Chem
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors. [Abstract]2024 Sep 12:107765. PMID: 39276936 -
bioRxiv
Hammerhead-type FXR agonists induce an eRNA FincoR that ameliorates nonalcoholic steatohepatitis in mice. [Abstract]2024 Feb 8:2023.11.20.567833. PMID: 38045226
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (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.
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.
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 KB)
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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 | 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 |
Tropifexor Related Classifications
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