An FXR agonist
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Tropifexor

Item No. 25748

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(3-endo)-3-[[5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-4-isoxazolyl]methoxy]-8-azabicyclo[3.2.1]oct-8-yl]-4-fluoro-6-benzothiazolecarboxylic acid
CAS Number
1383816-29-2
Synonyms
  • LJN452
Molecular Formula
C29H25F4N3O5S
Formula Weight
603.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/ml
λmax
313 nm
SMILES
FC1=C2C(SC(N3[C@H]4CC[C@@H]3C[C@H](OCC5=C(C6CC6)ON=C5C7=CC=CC=C7OC(F)(F)F)C4)=N2)=CC(C(O)=O)=C1
InChi Code
InChI=1S/C29H25F4N3O5S/c30-21-9-15(27(37)38)10-23-25(21)34-28(42-23)36-16-7-8-17(36)12-18(11-16)39-13-20-24(35-41-26(20)14-5-6-14)19-3-1-2-4-22(19)40-29(31,32)33/h1-4,9-10,14,16-18H,5-8,11-13H2,(H,37,38)/t16-,17+,18+
InChi Key
VYLOOGHLKSNNEK-PIIMJCKOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    Tropifexor is an agonist of farnesoid X receptors (FXR).1 It enhances the interaction between the human FXR ligand binding domain and the steroid receptor coactivator 1 (SRC-1) peptide in a homogeneous time-resolved fluorescence (HTRF) coactivator interaction assay (EC50 = 0.2 nM). It increases expression of the FXR target genes BSEP and SHP and decreases expression of CPY8B1 in rat liver in a dose-dependent manner, as well as increases expression of SHP and FGF15 in rat ileum. Tropifexor (0.3 mg/kg) reduces triglyceride levels by 79% in rat serum. It reduces fibrosis, inflammation, and steatosis in a mouse model of nonalcoholic steatohepatitis (NASH).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tully, D.C., Rucker, P.V., Chianelli, D., et al. Discovery of tropifexor (LJN452), a highly potent non-bile acid FXR agonist for the treatment of cholestatic liver diseases and nonalcoholic steatohepatitis (NASH). J. Med. Chem. 60(24), 9960-9973 (2017).

    2. Laffitte, B., Hernandez, E., Kim, Y., et al. THU-468 - LJN452 (tropifexor) attenuates steatohepatitis, inflammation, and fibrosis in dietary mouse models of nonalcoholic steatohepatitis. J. Hepatol. 68(Suppl 1), S341-S342 (2018).