Tropifexor (LJN452)

Catalog No.S8733 Batch:S873301

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Technical Data

Formula

C29H25F4N3O5S
Molecular Weight 603.58 CAS No. 1383816-29-2
Solubility (25°C)* In vitro DMSO 100 mg/mL (165.67 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Animal Study:

[1]
  • Animal Models

    Adult male wild-type Sprague-Dawley rats

  • Dosages

    0.03, 0.1, 0.3, and 1.0 mg/kg

  • Administration

    oral administration

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.