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Tropifexor

Catalog No. T4379Cas No. 1383816-29-2
Alias LJN452

Tropifexor (LJN452) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.

Tropifexor

Tropifexor

Purity: 99.85%
Catalog No. T4379Alias LJN452Cas No. 1383816-29-2
Tropifexor (LJN452) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
Pack SizePriceAvailabilityQuantity
1 mg$89In Stock
5 mg$169In Stock
10 mg$261In Stock
25 mg$460In Stock
50 mg$700In Stock
100 mg$1,060In Stock
200 mg$1,600In Stock
500 mg$2,370In Stock
1 mL x 10 mM (in DMSO)$225In Stock
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Purity:99.85%
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Product Introduction

Bioactivity
Description
Tropifexor (LJN452) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
Targets&IC50
FXR:EC50: 0.2 nM
In vitro
Robust induction of both BSEP and SHP genes is observed in primary cells by Tropifexor in a concentration-dependent manner. BSEP induction above vehicle (DMSO) control is observed at concentrations as low as 1 nM, while strong induction of SHP (15-fold above vehicle) is observed at 10 nM and modest induction of SHP at 1 nM (3-fold).
In vivo
Treatment of rats with Tropifexor exhibits a clear increase in plasma FGF15 protein in a dose-dependent manner, with maximal levels of FGF15 detected at 7 h postdose. Treatment with Tropifexor for 14 days results in a robust dose-dependent reduction in serum triglycerides and reaches a maximal response with a 0.3 mg/kg dose, causing a decrease of triglyceride levels to approximately 79% below the vehicle control group. Tropifexor (compound 1) demonstrates highly potent induction of SHP and FGF15 in the ileum as doses as low as 0.1 mg/kg. In the liver, robust induction of SHP is observed at 0.01 mg/kg of Tropifexor with maximal levels of gene induction achieved at 0.3 mg/kg. Expression of CYP8B1 mRNA following 14 day treatment with Tropifexor is already apparent at the lowest dose (0.003 mg/kg), and CYP8B1 gene expression is fully repressed at doses above 0.03 mg/kg.
Cell Research
Primary rat hepatocytes are plated in 24 well plates and incubated with a 5 point dose response of Tropifexor (compound 1) for 24 hours. RNA is harvested from the cells using the RNeasy 96 kit. Quantitative PCR is performed. The fold change of the transcript over no stimulation is calculated using the ΔΔCt method, with DMSO (vehicle control) being no stimulation.
Animal Research
Adult male wild-type Sprague-Dawley rats are used in this study. All animals are fasted for 3 hours before oral dosing with Tropifexor (compound 1) or with vehicle. Tropifexor is administered orally using a range of four doses (0.03, 0.1, 0.3, and 1.0 mg/kg) and compare directly to the vehicle control group (vehicle: 0.5% methylcellulose, 0.5% Tween 80, 99% water, suspension). Animals are sacrificed seven hours after dosing using CO2, liver, ileum and whole blood (in heparinized tubes) samples are collected for analysis.
AliasLJN452
Chemical Properties
Molecular Weight603.58
FormulaC29H25F4N3O5S
Cas No.1383816-29-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (82.84 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6568 mL8.2839 mL16.5678 mL82.8391 mL
5 mM0.3314 mL1.6568 mL3.3136 mL16.5678 mL
10 mM0.1657 mL0.8284 mL1.6568 mL8.2839 mL
20 mM0.0828 mL0.4142 mL0.8284 mL4.1420 mL
50 mM0.0331 mL0.1657 mL0.3314 mL1.6568 mL

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