Home Metabolism FXR agonist Tropifexor (LJN452) For research use only.

Tropifexor (LJN452)

Tropifexor (LJN452) is a novel and highly potent agonist of FXR with EC50 of 0.2 nM in HTRF assay. It shows no significant off-target activity against a broad panel of enzyme, ion channel, nuclear receptor, and GPCR (>10000-fold selectivity for FXR).

Tropifexor (LJN452) Chemical Structure

Tropifexor (LJN452) Chemical Structure

CAS No. 1383816-29-2

Purity & Quality Control

Batch: S873301 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.32%
99.32

Tropifexor (LJN452) Related Products

Biological Activity

Description Tropifexor (LJN452) is a novel and highly potent agonist of FXR with EC50 of 0.2 nM in HTRF assay. It shows no significant off-target activity against a broad panel of enzyme, ion channel, nuclear receptor, and GPCR (>10000-fold selectivity for FXR).
Targets
FXR [1]
(HTRF assay)
0.2 nM(EC50)
In vitro
In vitro

LJN-452 in in vitro pharmacological studies has shown to be a potent human FXR agonist with > 30,000-fold selectivity over other nuclear receptors[2]. LJN-452 could increases BSEP and SHP expression in primary human hepatocyte[3].
In Vivo
In vivo

Tropifexor has low clearance (CL = 9 mL/min/kg) and a significantly longer terminal half-life (T1/2 = 3.7 h) in rat pharmacokinetics. Oral bioavailability of tropifexor in the rat is 20% from an aqueous microemulsion formulation. In the mouse, following IV administration, Tropifexo exhibits low clearance and small volume of distribution with a half-life of 2.6 h. In the dog, following IV injection, the clearance was low and T1/2 was 7.4 h, also with a small volume of distribution (0.46 L/kg)[1]. Preclinical data demonstrate a dose-dependent increase in fibroblast growth factor 19 (FGF-19) levels with LJN-452, in single-dose or multiple-dose studies, with its target engagement in enterocyte FXRs[2]. Tropifexor improves liver transaminases and fibrosis in the ANIT model[3].
Animal Research Animal Models Adult male wild-type Sprague-Dawley rats
Dosages 0.03, 0.1, 0.3, and 1.0 mg/kg
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04408937 Completed
Liver Disease
Novartis Pharmaceuticals|Novartis
 May 29 2020 Phase 1
NCT02855164 Terminated
Non-alcoholic Steatohepatitis (NASH)
Novartis Pharmaceuticals|Novartis
 August 1 2016 Phase 2
NCT02713243 Completed
Primary Bile Acid Diarrhea
Novartis Pharmaceuticals|Novartis
 January 16 2016 Phase 2

Chemical Information & Solubility

Molecular Weight 603.58 Formula

C29H25F4N3O5S
CAS No. 1383816-29-2 SDF --
Smiles C1CC1C2=C(C(=NO2)C3=CC=CC=C3OC(F)(F)F)COC4CC5CCC(C4)N5C6=NC7=C(C=C(C=C7S6)C(=O)O)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (165.67 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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