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Lithocholic Acid (Synonyms: 3α-hydroxy Cholanic Acid, LCA, Lithocholate, NSC 683770)

Catalog No.GC17057

Activator of vitamin D receptor,PXR and FXR

Products are for research use only. Not for human use. We do not sell to patients.

Lithocholic Acid Chemical Structure

Cas No.: 434-13-9

Size Price Stock Qty
10mM (in 1mL DMSO)
$36.00
In stock
500mg
$29.00
In stock
1g
$43.00
In stock
5g
$69.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

HL-1 cells

Preparation method

The solubility of this compound in DMSO is > 13 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

50 or 100 μM

Applications

In HL-1 cells, Lithocholic Acid reduced and prevented cardiomyocyte apoptosis at the concentrations of 50 and 100 μM, respectively. In the presences of the pro-apoptotic stimulus, Doxazosin, Lithocholic Acid inhibited hyperphosphorylation of EphA2. In addition, Lithocholic Acid increased the expression of total EphA2.

Animal experiment [2]:

Animal models

Mice

Dosage form

0.125 mg/g; i.p.; b.i.d., for 4 days.

Applications

In PXR-/- mice, Lithocholic Acid resulted in sticky residues. Analysis of the urine revealed that PXR-/- mice showed substantially increased levels of Lithocholic Acid compared with wild-type animals. In addition, wild-type mice treated with Lithocholic Acid in a shorter term showed significant increases in hepatic Cyp3a11 and Oatp2 expression, whereas Lithocholic Acid treatment exhibited no effect on the expression of those genes in PXR-/- mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Jehle J, Staudacher I, Wiedmann F, Schweizer P, Becker R, Katus H, Thomas D. Regulation of apoptosis in HL-1 cardiomyocytes by phosphorylation of the receptor tyrosine kinase EphA2 and protection by lithocholic acid. Br J Pharmacol. 2012 Dec;167(7):1563-72.

[2]. Staudinger JL, Goodwin B, Jones SA, Hawkins-Brown D, MacKenzie KI, LaTour A, Liu Y, Klaassen CD, Brown KK, Reinhard J, Willson TM, Koller BH, Kliewer SA. The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3369-74.

Background

Lithocholic acid (LCA) is a toxic secondary bile acid, causing intrahepatic cholestasis, which has tumor-promoting activity.

In vitro: Among 17 kinds of bile acids with respect to inhibition of mammalian DNA polymerases, only LCA and its derivatives inhibited DNA polymerases, while other bile acids did not show inhibitory effect [1].

In vivo: Administration of LCA and its conjugates to rodents causes intrahepatic cholestasis, which is a pathogenic state characterized by decreased bile flow and the accumulation of bile constituents in the liver and blood [2].

Clinical trials: Currently no clinical data are available.

References:
[1] Ogawa A, Murate T, Suzuki M, Nimura Y, Yoshida S.  Lithocholic acid, a putative tumor promoter, inhibits mammalian DNA polymerase beta. Jpn J Cancer Res. 1998 Nov;89(11):1154-9.
[2] Staudinger JL, Goodwin B, Jones SA, Hawkins-Brown D, MacKenzie KI, LaTour A, Liu Y, Klaassen CD, Brown KK, Reinhard J, Willson TM, Koller BH, Kliewer SA.  The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3369-74.

Chemical Properties

Cas No. 434-13-9 SDF
Synonyms 3α-hydroxy Cholanic Acid, LCA, Lithocholate, NSC 683770
Chemical Name (4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
Canonical SMILES CC(CCC(=O)O)C1CCC2C1(CCC3C2CCC4C3(CCC(C4)O)C)C
Formula C24H40O3 M.Wt 376.57
Solubility ≥ 12.95mg/mL in DMSO Storage Store at 4°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6555 mL 13.2777 mL 26.5555 mL
5 mM 0.5311 mL 2.6555 mL 5.3111 mL
10 mM 0.2656 mL 1.3278 mL 2.6555 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 14 reference(s) in Google Scholar.)

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