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Tropifexor

Chemical Structure : Tropifexor

CAS No.: 1383816-29-2

Tropifexor (LJN-452;LJN452)

Catalog No.: PC-60056Not For Human Use, Lab Use Only.

Tropifexor (LJN-452, LJN452) is a novel highly potent, selective, orally acitive FXR full agonist with EC50 of 0.26 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Tropifexor (LJN-452, LJN452) is a novel highly potent, selective, orally acitive FXR full agonist with EC50 of 0.26 nM.
Tropifexor (LJN-452, LJN452) shows no significant off-target activity (>10,000-fold selectivity for FXR) in a panel of targets, including TGR5 (>10 uM).
Tropifexor (LJN-452, LJN452) demonstrates in vivo activity in rodent PD models, and shows potential for treatment of cholestatic liver diseases and NASH.

Physicochemical Properties

M.Wt 603.589
Formula C29H25F4N3O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Tully DC, et al. J Med Chem. 2017 Dec 8. doi: 10.1021/acs.jmedchem.7b00907.

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