2. Metabolic Enzyme/Protease
  3. FXR
  4. FXR antagonist 1

FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies.

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FXR antagonist 1 Chemical Structure

FXR antagonist 1 Chemical Structure

CAS No. : 2295804-68-9

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Based on 1 publication(s) in Google Scholar

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FXR antagonist 1 Related Antibodies

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Description

FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies[1].

IC50 & Target[1]

FXR

2.1 μM (IC50)

In Vitro

FXR antagonist 1 (0-100 µM; 24 h) shows FXR antagonistic activities in HEK293T cells[1].

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

FXR antagonist 1 Related Antibodies

Cell Viability Assay[1]

Cell Line: HEK293T cells (co-transfected with pCMV-Script-hFXR and pGL4.11-hSHP-Luciferase)
Concentration: 0-100 µM
Incubation Time: 24 h
Result: Exhibited FXR antagonistic activities with an IC50 value of 2.1 μM.
In Vivo

FXR antagonist 1 (10 mg/kg; p.o.; single daily for 12 weeks) reduces adiposity and improves glucose sensitivity and ameliorates the progress of NASH in GAN-diet-induced NASH mice[1].
FXR antagonist 1 (10 mg/kg; p.o.; single daily for 12 weeks) inhibits intestinal FXR Signaling but indirectly activates hepatic FXR signaling in GAN-diet-induced mice[1].
FXR antagonist 1 (3, 10, 30 mg/kg; p.o.; single daily for 4 weeks) dose-dependently alleviates NASH pathologies in HFMCD-diet-induced mice[1].

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

Animal Model: Adult male C57BL/6 mice (GAN (Gubra-amylin NASH)-diet induced NASH model)[1].
Dosage: 10 mg/kg
Administration: Oral administration; single daily for 12 weeks.
Result: Reversed metabolic dysfunction in GAN-induced NASH mice.
Reduced GAN-diet-induced hepatic steatosis, injury, inflammation, and fibrosis.
Inhibited the hepatic mRNA expression involved in lipid metabolism, inflammatory signaling, and fibrogenesis in GAN-diet-induced mice.
Significantly antagonized intestinal FXR signaling and bile acid reabsorption.
Animal Model: Adult male C57BL/6 mice (HFMCD-diet induced NASH model)[1].
Dosage: 3, 10, 30 mg/kg
Administration: Oral administration; single daily for 4 weeks.
Result: Significantly decreased serum ALT and AST levels at 30 mg/kg, and markedly lowered the hepatic TG concentration in both 10 and 30 mg/kg.
Lowered hepatic hydroxyproline level.
Molecular Weight

585.86

Formula

C36H59NO5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(CNC([C@]12[C@@]([C@@H](CC2)C(C)C)([H])[C@]3([H])[C@@](CC1)([C@]4([C@]([C@@]5([C@@](C(C)([C@@H](CC5)OC(CCC)=O)C)([H])CC4)C)([H])CC3)C)C)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (170.69 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 1.7069 mL 8.5345 mL 17.0689 mL
5 mM 0.3414 mL 1.7069 mL 3.4138 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (4.27 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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 (4.27 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. 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:

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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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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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7069 mL 8.5345 mL 17.0689 mL 42.6723 mL
5 mM 0.3414 mL 1.7069 mL 3.4138 mL 8.5345 mL
10 mM 0.1707 mL 0.8534 mL 1.7069 mL 4.2672 mL
15 mM 0.1138 mL 0.5690 mL 1.1379 mL 2.8448 mL
20 mM 0.0853 mL 0.4267 mL 0.8534 mL 2.1336 mL
25 mM 0.0683 mL 0.3414 mL 0.6828 mL 1.7069 mL
30 mM 0.0569 mL 0.2845 mL 0.5690 mL 1.4224 mL
40 mM 0.0427 mL 0.2134 mL 0.4267 mL 1.0668 mL
50 mM 0.0341 mL 0.1707 mL 0.3414 mL 0.8534 mL
60 mM 0.0284 mL 0.1422 mL 0.2845 mL 0.7112 mL
80 mM 0.0213 mL 0.1067 mL 0.2134 mL 0.5334 mL
100 mM 0.0171 mL 0.0853 mL 0.1707 mL 0.4267 mL
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FXR antagonist 1 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:

FXR antagonist 12295804-68-9FXR antagonist1FXR antagonist-1FXRNR1H4NASHHEK293TGANhepatic steatosishepatic inflammationhepatic fibrosisInhibitorinhibitorinhibit

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