Tropifexor (LJN452)

Catalog No.S8733

Tropifexor (LJN452) Chemical Structure

Molecular Weight(MW): 603.58

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).

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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

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

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].

Protocol

Animal Research:

[1]

- Collapse
  • Animal Models: Adult male wild-type Sprague-Dawley rats
  • Formulation: 0.5% methylcellulose, 0.5% Tween80, 99% water, suspension
  • Dosages: 0.03, 0.1, 0.3, and 1.0 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (165.67 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 603.58
Formula

C29H25F4N3O5S

CAS No. 1383816-29-2
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID