A major metabolite of lithocholic acid; formed from LCA by CYP3A4; an agonist of TGR5 (EC50 = 0.27 μM)

Dehydrolithocholic Acid – 250 mg

Brand:
Cayman
CAS:
1553-56-6
Storage:
-20
UN-No:
Non-Hazardous - /

Dehydrolithocholic acid is a major metabolite of lithocholic acid (LCA; Item No. 20253).{48226} It is formed from LCA by the cytochrome P450 (CYP) isoform CYP3A4. Dehydrolithocholic acid is an agonist of G protein-coupled bile acid activated receptor 1 (GP-BAR1/TGR5; EC50 = 0.27 μM), vitamin D receptor (VDR; EC50 = 3 μM), and farnesoid X receptor (FXR) in cell-based reporter assays.{53582,10150} It also binds to the human pregnane X receptor (PXR; IC50 = 15 μM) and activates mouse and human PXRs in cell-based reporter assays when used at a concentration of 100 μM.{32396} Dehydrolithocholic acid binds to retinoic acid receptor-related orphan receptor γt (RORγt; Kd = 1.13 μM for the recombinant human ligand-binding domain) and decreases its activity in a cell-based reporter assay when used at a concentration of 10 μM.{53583} It inhibits the differentiation of T helper cells that express IL-17a (TH17 cells) when used at a concentration of 20 μM.  

 

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Description

A major metabolite of lithocholic acid; formed from LCA by CYP3A4; an agonist of TGR5 (EC50 = 0.27 μM), VDR (EC50 = 3 μM), and FXR in cell-based reporter assays; binds to human PXR (IC50 = 15 μM) and activates mouse and human PXRs in cell-based reporter assays at 100 μM; binds to RORγt (Kd = 1.13 μM for the recombinant human ligand-binding domain) and decreases its activity in a cell-based reporter assay at 10 μM; inhibits the differentiation of TH17 cells at 20 μM

Formal name: (5β)-3-oxo-cholan-24-oic acid

Synonyms:  3-Ketolithocholic Acid|3-oxo Lithocholic Acid|3-oxoLCA

Molecular weight: 374.6

CAS: 1553-56-6

Purity: ≥95%

Formulation: A crystalline solid

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