An FXR agonist; enhances the interaction between the human FXR ligand binding domain and the SRC-1 peptide in an HTRF coactivator interaction assay (EC50 = 0.2 nM); increases expression of the FXR target genes BSEP and SHP and decreases expression of CPY8B1 in rat liver in a dose-dependent manner

Tropifexor – 500 µg

Brand:
Cayman
CAS:
1383816-29-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Tropifexor is an agonist of farnesoid X receptors (FXR).{48126} 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).{48127}  

 

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SKU: 25748 - 500 µg Category:

Description

An FXR agonist; enhances the interaction between the human FXR ligand binding domain and the SRC-1 peptide in an HTRF coactivator interaction assay (EC50 = 0.2 nM); 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; reduces triglyceride levels by 79% in rat serum at 0.3 mg/kg; reduces fibrosis, inflammation, and steatosis in a mouse model of NASH

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

Synonyms:  LJN452

Molecular weight: 603.6

CAS: 1383816-29-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Bile Acids & Microbiome||Research Area|Endocrinology & Metabolism|Hormones & Receptors|FXRs & LXRs||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Dyslipidemias||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH

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