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Lithocholic acid


CAS No. : 434-13-9

(Synonyms: 3α-Hydroxy-5β-cholanic acid)

434-13-9
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Cat. No. : HY-B0172
M.Wt: 376.57
Formula: C24H40O3
Purity: >98 %
Solubility: Ethanol : 10 mg/mL (ultrasonic;warming;heat to 60°C);DMSO : 100 mg/mL (ultrasonic);H2O : 0.99 mg/mL (ultrasonic;warming;adjust pH to 11 with NaOH;heat to 60°C)
Introduction of 434-13-9 :

Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist[1][2][3][4][5]. In Vitro:Lithocholic acid inhibits CDCA- and GW4064-induced FXR activation with an IC50of 0.7 and 1.4 μM, respectively[5].
Lithocholic acid (10-30 μM, 24 h) inhibits the 100 nM GW4064 induced BSEP expression in HepG2 cells[5].
Lithocholic acid (0-500 μM) dose-dependently inhibits the proliferation of neuroblastoma cells (BE(2)-m17, SK-n-SH, SK-n-MCIXC and Lan-1)[3].
In Vivo:Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Lithocholic acid (LCA) can be used to induce cholestasis models[6][7].

Induction of cholestasis[6][7]
Background
LCA has certain toxicity to hepatocytes, which can change bile secretion through its osmotic effect and cause cholestasis by changing the cell membrane components of hepatocytes that are rich in bile duct membranes.
Specific Modeling Methods
Rat: Wistar • male • 250 ~ 300 g (period: 1 h)
Administration: 0.2 μmol/100 g • iv • killed after 1 h
Mice: ICR • male • 5-7-week-old (period: 3 days)
Administration: 150 mg/kg • po • 2 times a day for 5 times
Note
(1) LCA (i.v.) is taken up in 7.5% bovine serum albumin and 0.45% saline.
(2) LCA (p.o.) is taken up in corn oil. The animals were sacrificed 12 h following the 5th treatment. The blood samples (50 μl) can be collected by tail bleeding at 0, 12, 24 and 36 h following the 1st dose.
Modeling Indicators
Histological changes: There was a significant increase in bile flow shortly after LCA injection, after which bile flow decreased significantly. Pathological changes can be observed in liver tissue, including liver necrosis and diffuse vacuoles.

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