Fexaramine
Based on 10 publication(s) in Google Scholar
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.
- Purity: 99.20%
- CAS No.: 574013-66-4
- Formula: C32H36N2O3
- Molecular Weight:496.64
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Autophagy Compound Library
HY-L029
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Human Metabolite Library
HY-L123
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Nuclear Receptor Compound Library
HY-L126
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Mass Spectrometry Human Metabolite Library
HY-L215
Publications Citing Use of MedChemExpress (MCE) Fexaramine
More- Cell Host Microbe. 2024 Feb 14;32(2):191-208.e9. [Abstract]
- Nat Commun. 2023 Oct 30;14(1):6908. [Abstract]
- Adv Sci (Weinh). 2024 Dec 16:e2406445. [Abstract]
- J Adv Res. 2026 Mar 12:S2090-1232(26)00239-0. [Abstract]
- MedComm. 2024 Apr 25;5(5):e556. [Abstract]
- NPJ Biofilms Microbiomes. 2026 Jan 8;12(1):38. [Abstract]
- J Agric Food Chem. 2023 Jan 11;71(1):867-876. [Abstract]
- Int J Mol Med. 2018 Sep;42(3):1723-1731. [Abstract]
- Mech Ageing Dev. 2022 Mar:202:111630. [Abstract]
- bioRxiv. 2024 Feb 8:2023.11.20.567833. [Abstract]
Customer Validation & Images
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WB
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Histological Imaging/Staining
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RT-PCR
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Flow Cytometry
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Cell Imaging/Staining
Biological Activity
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.
Chemical Information
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CAS No. 574013-66-4
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Appearance Solid
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Molecular Weight 496.64
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Formula C32H36N2O3
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Color Light yellow to yellow
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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
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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 (10)
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Journal Impact Factor
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Most Recent
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Cell Host Microbe
A gut microbiota-bile acid axis promotes intestinal homeostasis upon aspirin-mediated damage. [Abstract]2024 Feb 14;32(2):191-208.e9. PMID: 38237593 -
Nat Commun
Farnesoid X receptor activation by bile acids suppresses lipid peroxidation and ferroptosis. [Abstract]2023 Oct 30;14(1):6908. PMID: 37903763
Fexaramine purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 30;14(1):6908. [Abstract]
Treatment of HT-1080 with 12 µM Turofexorate or Fexaramine for 7 h increases FXR expression. Levels of mRNA were normalized to GAPDH expression.
Fexaramine purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 30;14(1):6908. [Abstract]
FXR activation by 12 µM Turofexorate or Fexaramine reduces 4-HNE levels. Ferroptosis was induced by 300 nM RSL3 for 2 h. 2 µM Fer-1 was used as positive control. Representative flow cytometry histogram is shown.
Fexaramine purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 30;14(1):6908. [Abstract]
HT-1080 3D spheroid models are rescued from ferroptosis by treatment with 12 µM Turofexorate or Fexaramine for 48 h. Ferroptosis was induced by 200 nM RSL3 for 48 h, 2 µM Fer-1 was used as a positive control. Representative spheroid images are shown.
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Adv Sci (Weinh)
Clostridium Scindens Protects Against Vancomycin-Induced Cholestasis and Liver Fibrosis by Activating Intestinal FXR-FGF15/19 Signaling. [Abstract]2024 Dec 16:e2406445. PMID: 39680750
Fexaramine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Dec 16:e2406445. [Abstract]
Representative immunoblots of CYP7A1 in liver tissue treated with Fexaramine (Fex).
Fexaramine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Dec 16:e2406445. [Abstract]
Representative images of liver specimens stained with hematoxylin and eosin treated with Fexaramine (Fex).
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J Adv Res
Conjugated bile acids facilitate cholangiocyte senescence to promote cholestatic liver diseases via STING signaling. [Abstract]2026 Mar 12:S2090-1232(26)00239-0. PMID: 41831676 -
MedComm
Mineral crude drug mirabilite (Mangxiao) inhibits the occurrence of colorectal cancer by regulating the Lactobacillus-bile acid-intestinal farnesoid X receptor axis based on multiomics integration analysis. [Abstract]2024 Apr 25;5(5):e556. PMID: 38665997 -
NPJ Biofilms Microbiomes
Disruption of bile acid homeostasis potentiates Paneth cell ablation by activating the intestinal Farnesoid X receptor in necrotizing enterocolitis. [Abstract]2026 Jan 8;12(1):38. PMID: 41507219 -
J Agric Food Chem
Aflatoxin B1 Induces Intestinal Barrier Dysfunction by Regulating the FXR-Mediated MLCK Signaling Pathway in Mice and in IPEC-J2 Cells. [Abstract]2023 Jan 11;71(1):867-876. PMID: 36579420 -
Int J Mol Med
Farnesoid X receptor agonist decreases lipid accumulation by promoting hepatic fatty acid oxidation in db/db mice. [Abstract]2018 Sep;42(3):1723-1731. PMID: 29901078 -
Mech Ageing Dev
2022 Mar:202:111630. PMID: 35026209 -
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 : 50 mg/mL (100.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (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.
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lam IP, et al. Bile acids inhibit duodenal secretin expression via orphan nuclear receptor small heterodimer partner (SHP). Am J Physiol Gastrointest Liver Physiol. 2009 Jul;297(1):G90-7. [Content Brief]
[2]. Michael Downes, et al. A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. Mol Cell. 2003 Apr;11(4):1079-92. [Content Brief]
[3]. Fang S, et al. Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance. Nat Med. 2015 Feb;21(2):159-65. [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, 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 |
Fexaramine Related Classifications
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