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: 1383816-29-2

Purity & Quality Control

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

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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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