Art. -Nr.: HY-10912

Fexaramine

10 Cited Publications

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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.

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Reinheit: 99.20%
CAS. Nr.: 574013-66-4
Formel: C₃₂H₃₆N₂O₃
Molecular Weight:496.64

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Fexaramine Chemical Structure

CAS. Nr.: 574013-66-4

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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.

Chemical Information

CAS. Nr. 574013-66-4
Appearance Solid
Molecular Weight 496.64
Formel C₃₂H₃₆N₂O₃
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (10)

All WBRT-PCRHistological Imaging/StainingFlow CytometryCell Imaging/Staining

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Journal Impact Factor

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.
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
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).
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
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
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
Mech Ageing Dev

Ileal FXR-FGF15/19 signaling activation improves skeletal muscle loss in aged mice. [Abstract]

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0135 mL

10.0677 mL

20.1353 mL

5 mM

0.4027 mL

2.0135 mL

4.0271 mL

10 mM

0.2014 mL

1.0068 mL

2.0135 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.03 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Fexaramine

10 Cited Publications

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Fexaramine

Metabolism/Protease Compound Library

Autophagy Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Fexaramine

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Fexaramine

Metabolism/Protease Compound Library

Autophagy Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Fexaramine

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Fexaramine Related Classifications

HY-10912 Related Classifications