Cat. No.: HY-151481

FXR antagonist 1

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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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Pureté: 99.85%
CAS No.: 2295804-68-9
Formule: C₃₆H₅₉NO₅
Masse moléculaire:585.86

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

FXR antagonist 1 Chemical Structure

CAS No.: 2295804-68-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

FXR

2.1 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	>100 μM Compound: F6	Cytotoxicity against HEK293T cells cotransfected with pCMV-Script-hFXR/pGL4.11-hSHP-Luciferase incubated for 24 hrs in presence of GW4064 by celltiter-blue cell viability assay Cytotoxicity against HEK293T cells cotransfected with pCMV-Script-hFXR/pGL4.11-hSHP-Luciferase incubated for 24 hrs in presence of GW4064 by celltiter-blue cell viability assay	[PMID: 36107013]

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.

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.

Chemical Information

CAS No. 2295804-68-9
Appearance Solid
Masse moléculaire 585.86
Formule C₃₆H₅₉NO₅
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

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)

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

1.7069 mL

8.5345 mL

17.0689 mL

5 mM

0.3414 mL

1.7069 mL

3.4138 mL

10 mM

0.1707 mL

0.8534 mL

1.7069 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, 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: 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.

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:

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instruction de manipulation (2659 KB)

Références

[1]. Zhang C, et al. Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis. J Med Chem. 2022 Sep 15. [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, 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

Bioactive Compound Library Max

Bioactive Compound Library

Metabolism/Protease Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

MCE Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

FXR antagonist 1

Bioactive Compound Library Max

Bioactive Compound Library

Metabolism/Protease Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

MCE Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

FXR antagonist 1 Related Classifications

HY-151481 Related Classifications