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FXR agonist 3

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Catalog No. T74996

FXR agonist 3 is an anti-NASH compound with antifibrotic and anti-fibrotic activity, inhibiting the expression of COL1A1, TGF-β1, α-SMA, and TIMP1, with an IC50 value of 8.19 μmol/L for COL1A1. FXR agonist 3 ameliorates CDAHFD and BDL-induced liver injury in vivo by activating FXR.

FXR agonist 3

FXR agonist 3

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Purity: 95.04%
Catalog No. T74996
FXR agonist 3 is an anti-NASH compound with antifibrotic and anti-fibrotic activity, inhibiting the expression of COL1A1, TGF-β1, α-SMA, and TIMP1, with an IC50 value of 8.19 μmol/L for COL1A1. FXR agonist 3 ameliorates CDAHFD and BDL-induced liver injury in vivo by activating FXR.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$99-In Stock
5 mgPreferential-In Stock
1 mL x 10 mM (in DMSO)$599-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:95.04%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
FXR agonist 3 is an anti-NASH compound with antifibrotic and anti-fibrotic activity, inhibiting the expression of COL1A1, TGF-β1, α-SMA, and TIMP1, with an IC50 value of 8.19 μmol/L for COL1A1. FXR agonist 3 ameliorates CDAHFD and BDL-induced liver injury in vivo by activating FXR.
In vitro
In LX-2 cells, FXR agonist 3 (0, 2.5, 5, 7.5, and 10 μM; 24 hours; with or without 2 ng/mL TGF-β1 for another 24 hours) decreased COL1A1, TGF-β1, α-SMA, and TIMP1 protein expressions in a dose-dependent manner[1].
In vivo
In C57BL/6 N mice fed a CDAHFD diet for 16 weeks, FXR agonist 3 (200 mg/kg; oral gavage; daily for 4 weeks after CDAHFD-induced) decreased the expression of IL-1β and IL-6 in the liver[1].
Chemical Properties
Molecular Weight521.12
FormulaC28H28BrNO4
SmilesCOC1=CC2=C(C=C1OC)CC[N+]3=C2C=C4C(C(OCC5=CC=CC(C)=C5)=C(OC)C=C4)=C3.[Br-]
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 200 mg/mL (383.79 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9189 mL9.5947 mL19.1894 mL95.9472 mL
5 mM0.3838 mL1.9189 mL3.8379 mL19.1894 mL
10 mM0.1919 mL0.9595 mL1.9189 mL9.5947 mL
20 mM0.0959 mL0.4797 mL0.9595 mL4.7974 mL
50 mM0.0384 mL0.1919 mL0.3838 mL1.9189 mL
100 mM0.0192 mL0.0959 mL0.1919 mL0.9595 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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