Information 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). Targets FXR (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. LJN-452 could increases BSEP and SHP expression in primary human hepatocyte. In vivo Tropifexor has low clearance (CL = 9 mL/min/kg) and a significantly longer terminal half-life (T 1/2 = 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 T 1/2 was 7.4 h, also with a small volume of distribution (0.46 L/kg). 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. Tropifexor improves liver transaminases and fibrosis in the ANIT model.
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Tropifexor (LJN452)
CAS number：1383816-29-2 molecular formula：C29H25F4N3O5S
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| Chinese alias | 特罗皮菲索 (LJN452) | ||
| English alias | AC-30341 | 2-[(1R,3r,5S)-3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazole-6-carboxylic acid | NMZ08KM76Z | WHO 10443 | 2-((1R,5S)-3-((5-cyclopropyl-3-(2-(trifluoromethoxy)p | ||
| CAS number | 1383816-29-2 | molecular formula | C29H25F4N3O5S |
| molecular weight | 603.58 g/mol | Exact mass | - |
| PSA | 126.000 Ų | logp | 6.8 |
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