1. Metabolic Enzyme/Protease
  2. FXR

Tropifexor (Synonyms: LJN452)

Cat. No.: HY-107418 Purity: 99.33%
Handling Instructions

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

For research use only. We do not sell to patients.
Tropifexor Chemical Structure

Tropifexor Chemical Structure

CAS No. : 1383816-29-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 940 In-stock
1 mg USD 228 In-stock
5 mg USD 708 In-stock
10 mg USD 1188 In-stock
50 mg USD 3588 In-stock
100 mg USD 4788 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

EC50: 0.2 nM (FXR)

In Vitro

Tropifexor (compound 1) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM. 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)[1].

In Vivo

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. Treatment of rats with Tropifexor exhibits a clear dose-dependent increase in plasma FGF15 protein, with maximal levels of FGF15 detected at 7 h postdose. Treatment with Tropifexor for 14 days produces a robust dose-dependent reduction in serum triglycerides and reaches a maximal response with a 0.3 mg/kg dose, resulting in a decrease of triglyceride levels to approximately 79% below the vehicle control group[1].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.6568 mL 8.2839 mL 16.5678 mL
5 mM 0.3314 mL 1.6568 mL 3.3136 mL
10 mM 0.1657 mL 0.8284 mL 1.6568 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

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[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

603.58

Formula

C₂₉H₂₅F₄N₃O₅S

CAS No.

1383816-29-2

SMILES

FC(F)(F)OC(C=CC=C1)=C1C2=NOC(C3CC3)=C2CO[[email protected]@H]4C[[email protected]]5N(C6=NC7=C(F)C=C(C(O)=O)C=C7S6)[[email protected]](CC5)C4

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.33%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Tropifexor
Cat. No.:
HY-107418
Quantity: