Home Metabolism FXR agonist Lithocholic acid For research use only.

Lithocholic acid

Lithocholic acid is a toxic secondary bile acid, causes intrahepatic cholestasis, has tumor-promoting activity, its toxic effect can be protected after it activates the vitamin D receptor, PXR and FXR.

CAS No. 434-13-9

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Biological Activity

Description Lithocholic acid is a toxic secondary bile acid, causes intrahepatic cholestasis, has tumor-promoting activity, its toxic effect can be protected after it activates the vitamin D receptor, PXR and FXR.
Targets
FXR [1] PXR [1] vitamin D receptor [1]
In vitro
In vitro

Lithocholic acid (LCA) is a hydrophobic secondary bile acid that is primarily formed in the intestine by the bacterial 7α-dehydroxylation of chenodeoxycholic acid. LCA causes intrahepatic cholestasis (cessation or impairment of bile flow). LCA activates PXR (pregnane X receptor), and the LCA-induced severe liver damage can be protected by the activation of PXR. [1] LCA can activate farnesoid X receptor (FXR) with EC50 of 3.8 μM. [2] LCA directly binds VDR (vitamin D receptor) with Ki of 29μM, activates VDR (vitamin D receptor) 30 μM, with much more sensitivity than the other nuclear receptors (eg. PXR, FXR), and its toxic effect is thus protected. [3] LCA has tumor-promoting activity, inhibits mammalian DNA Polymerase β with IC50 of 15 μM. [4]
Kinase Assay Competitive ligand binding assay.
Ligand binding is performed using lysates from COS-7 cells transfected with expression plasmids for VDR or RXRα. Binding is performed overnight at 4°C in lysate buffer with 0.71 nM (18 Ci/mmol) [3H]1,25(OH)2D3 and bile acid competitor. Unbound [3H]1,25(OH)2D3 is removed by adsorption to dextran-coated charcoal and the supernatant removed for scintillation counting. Ki values are calculated from a computer fit of competition curves from triplicate assays.
In Vivo
In vivo

Administration of LCA and its conjugates to rodents causes intrahepatic cholestasis,a pathogenic state characterized by decreased bile flow and the accumulation of bile constituents in the liver and blood. [1] In DMH (dimethyldydrazine)-induced murine carcinogenesis model, LCA suppresses apoptosis almost completely in premalignant colon. [5] LCA activates VDR, induces expression in vivo of CYP3A, a cytochrome P450 enzyme that detoxifies LCA in the liver and intestine. [3]
Animal Research Animal Models Mouse
Dosages 0.125 mg/g, twice a day for 4 days.
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02654496 Completed
Obesity
North Dakota State University
 January 2016 --
NCT01865812 Completed
Primary Biliary Cirrhosis
Intercept Pharmaceuticals
 December 3 2013 Phase 2

Chemical Information & Solubility

Molecular Weight 376.57 Formula

C24H40O3
CAS No. 434-13-9 SDF Download Lithocholic acid SDF
Smiles CC(CCC(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (199.16 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble


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