Molecular Formula | C29H25F4N3O5S |
Molar Mass | 603.58 |
Density | 1.55±0.1 g/cm3(Predicted) |
Boling Point | 700.0±65.0 °C(Predicted) |
pKa | 3.84±0.10(Predicted) |
Storage Condition | -20℃ |
In vitro study | LJN-452 in vitro pharmacological studies is a human FXR agonist, the selectivity of human FXR is more than 30,000 times higher than other nuclear receptors. In primary human hepatocytes, LJN-452 increased the expression levels of BSEP and SHP. |
In vivo study | Pharmacokinetic studies in rats showed that Tropifexor had a low clearance rate (CL = 9 ml/min/kg) and a long terminal Half-Life (T1/2=3.7 h). tropifexor was formulated as an aqueous microemulsion formulation with an oral bioavailability of 20% in rats. In mice, administered intravenously, Tropifexor has low clearance, small volume of distribution, and a half-life of 2.6 hours. In dogs, after intravenous injection, Tropifexor has a half-life of 7.4 hours and a volume of distribution of 0.46 L/kg. In single and multiple dose experiments, LJN-452 were able to target FXR in intestinal epithelial cells, resulting in a concentration-dependent increase in FGF-19 levels. In ANIT-induced liver injury model, Tropifexor can improve liver transaminases and fibrosis. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.657 ml | 8.284 ml | 16.568 ml |
5 mM | 0.331 ml | 1.657 ml | 3.314 ml |
10 mM | 0.166 ml | 0.828 ml | 1.657 ml |
5 mM | 0.033 ml | 0.166 ml | 0.331 ml |