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  4. Lithocholic acid

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

Cat. No.: HY-B0172 Purity: 99.96%
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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.

For research use only. We do not sell to patients.

CAS No. : 434-13-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of Lithocholic acid:

Top Publications Citing Use of Products

    Lithocholic acid purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb 3:e2411719.  [Abstract]

    The mRNA levels of ALDOB in Huh7 or HCCLM3 cells treated with various bile acids (100 μM, 24 h). All data are presented as mean ± SD. Data were analyzed by one-way ANOVA with Bonferroni multiple-comparison correction. CA, cholic acid; TCA, taurocholic acid; GCA, glycocholic acid; TCDCA, taurochenodeoxycholic acid; GCDCA, glycochenodeoxycholic acid; LCA, lithocholic acid; TLCA, taurolithocholic acid; GLCA, glycolithocholic acid; DCA, deoxycholic acid; TDCA, taurodeoxycholic acid; GDCA, glycodeoxycholic acid; UDCA, ursodeoxycholic acid; TUDCA, tauroursodeoxycholic acid; GUDCA, glycoursodeoxycholic acid.

    Lithocholic acid purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Oct:196:106902.  [Abstract]

    LCA supplementation ameliorated MCD-induced NASH aggravated by ALDH2 deficiency. Representative photomicrographs of liver sections stained with H&E or Oil-red O (scale bar, 100 μm); the NAS score and oil red O-positive area were analysed and quantified (n = 8).

    Lithocholic acid purchased from MedChemExpress. Usage Cited in: J Invest Dermatol. 2022 May;142(5):1381-1390.e11.

    (a) Schematic illustration of experimental protocols. Mice were administered i.v. PBS vehicle or LCA (Lithocholic acid, ) at a dose of 4 mg/kg/per day every other day beginning the following day after MC was delivered. (b) Percentage of baseline body weight, (c) representative photographs, (d) time course of ear thickness.

    Lithocholic acid purchased from MedChemExpress. Usage Cited in: J Invest Dermatol. 2022 May;142(5):1381-1390.e11.

    Wild-type C57BL/6 mice were administered i.v. PBS vehicle or LCA (Lithocholic acid ) at a dose of 4 mg/kg/per day every other day beginning the following day after MC was delivered.Image of H&E section (up), representative images of Ki-67 immunohistochemistry (bottom).

    Lithocholic acid purchased from MedChemExpress. Usage Cited in: Cell Res. 2019 Mar;29(3):193-205.  [Abstract]

    Effects of bile acids (BAs) on virus-induced transcription of antiviral genes. Raw264.7 cells were infected with HSV-1 or SeV for 30 min and treated with Lithocholic acid (LCA) (0.1 mM), Chenodeoxycholic Acid (CDCA) (0.1 mM) or Deoxycholic acid (DCA) (0.1 mM) for 6 h before qPCR analysis of the indicated mRNA levels.

    Lithocholic acid purchased from MedChemExpress. Usage Cited in: Cell Res. 2019 Mar;29(3):193-205.  [Abstract]

    Examination of intracellular bile acids (BA) levels after cells were treated with exogenous BAs. Raw264.7 cells were infected with HSV-1 or SeV for 30 min and treated with Lithocholic acid (LCA) (0.1 mM), Chenodeoxycholic Acid (CDCA) (0.1 mM) or Deoxycholic acid (DCA) (0.1 mM) for 6 h before BA assays were performed.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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].

    IC50 & Target

    Microbial Metabolite

     

    Human Endogenous Metabolite

     

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    > 200 μM
    Compound: LCA
    Anticancer activity against human A549 cells assessed as inhibition of cell proliferation by MTT assay
    Anticancer activity against human A549 cells assessed as inhibition of cell proliferation by MTT assay
    [PMID: 36439975]
    CHO EC50
    0.58 μM
    Compound: 6, LCA
    Agonist activity at human TGR5 expressed in CHO cells by luciferase assay
    Agonist activity at human TGR5 expressed in CHO cells by luciferase assay
    [PMID: 18307294]
    CHO EC50
    5.6 μM
    Compound: LCA
    Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
    Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
    [PMID: 19911773]
    COS-1 EC50
    20 μM
    Compound: 6, LCA
    Agonist activity at human FXR expressed in COS1 cells by luciferase assay
    Agonist activity at human FXR expressed in COS1 cells by luciferase assay
    [PMID: 18307294]
    COS-1 EC50
    6.7 μM
    Compound: LCA
    Agonist activity at human FXR expressed in COS1 cells by luciferase reporter gene assay
    Agonist activity at human FXR expressed in COS1 cells by luciferase reporter gene assay
    [PMID: 19911773]
    Caco-2 IC50
    56 μM
    Compound: LCA
    Cytotoxicity against human Caco2 cells assessed as cell viability after 24 hrs by MTT assay
    Cytotoxicity against human Caco2 cells assessed as cell viability after 24 hrs by MTT assay
    [PMID: 24332653]
    DLD-1 IC50
    173.1 μM
    Compound: LCA
    Cytotoxicity against human DLD1 cells assessed as cell viability after 48 hrs by MTT assay
    Cytotoxicity against human DLD1 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25685308]
    Erythrocyte IC50
    0.009 mg/mL
    Compound: L
    Hemolytic activity in human erythrocytes assessed as release of hemoglobin after 60 mins
    Hemolytic activity in human erythrocytes assessed as release of hemoglobin after 60 mins
    [PMID: 24461290]
    HCT-116 IC50
    81.1 μM
    Compound: LCA
    Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay
    Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25685308]
    HCT-116 IC50
    > 200 μM
    Compound: LCA
    Anticancer activity against human HCT-116 cells assessed as inhibition of cell proliferation by MTT assay
    Anticancer activity against human HCT-116 cells assessed as inhibition of cell proliferation by MTT assay
    [PMID: 36439975]
    HCT-8 IC50
    97.4 μM
    Compound: LCA
    Cytotoxicity against human HCT8 cells assessed as cell viability after 48 hrs by MTT assay
    Cytotoxicity against human HCT8 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25685308]
    HEK-293T EC50
    2.14 μM
    Compound: LCA
    Agonist activity at VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay
    Agonist activity at VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay
    [PMID: 26774929]
    HEK-293T IC50
    46.7 μM
    Compound: LCA
    Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay
    Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay
    [PMID: 26774929]
    HEK293 EC50
    0.68 μM
    Compound: 1, LCA
    Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
    Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
    [PMID: 25735208]
    HET-1A CC50
    25 μM
    Compound: 35, LCA
    Cytotoxicity against human HET-1A cells assessed as cell viability after 24 hrs by MTT assay
    Cytotoxicity against human HET-1A cells assessed as cell viability after 24 hrs by MTT assay
    [PMID: 20713311]
    HT-1080 IC50
    23 μM
    Compound: LCA
    Cytotoxicity against human HT1080 cells assessed as cell viability after 24 hrs by MTT assay
    Cytotoxicity against human HT1080 cells assessed as cell viability after 24 hrs by MTT assay
    [PMID: 24332653]
    HT-29 IC50
    > 200 μM
    Compound: LCA
    Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay
    Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay
    [PMID: 36439975]
    HepG2 EC50
    50 μM
    Compound: LCA
    Cytotoxicity in human HepG2 cells assessed as induction of cell necrosis incubated for 4 hrs by LDH release assay
    Cytotoxicity in human HepG2 cells assessed as induction of cell necrosis incubated for 4 hrs by LDH release assay
    [PMID: 27652492]
    HepG2 EC50
    50 μM
    Compound: LCA
    Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 4 hrs by CellTiter-Glo assay
    Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 4 hrs by CellTiter-Glo assay
    [PMID: 27652492]
    Huh-7 IC50
    > 200 μM
    Compound: LCA
    Anticancer activity against human Huh-7 cells assessed as inhibition of cell proliferation by MTT assay
    Anticancer activity against human Huh-7 cells assessed as inhibition of cell proliferation by MTT assay
    [PMID: 36439975]
    LoVo IC50
    > 200 μM
    Compound: LCA
    Anticancer activity against human LoVo cells assessed as inhibition of cell proliferation by MTT assay
    Anticancer activity against human LoVo cells assessed as inhibition of cell proliferation by MTT assay
    [PMID: 36439975]
    MGC-803 IC50
    > 200 μM
    Compound: LCA
    Anticancer activity against human MGC-803 cells assessed as inhibition of cell proliferation by MTT assay
    Anticancer activity against human MGC-803 cells assessed as inhibition of cell proliferation by MTT assay
    [PMID: 36439975]
    NCI-H716 EC50
    5 μM
    Compound: LCA
    Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
    Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
    [PMID: 24900463]
    PC-3 IC50
    50 μM
    Compound: 1, LCA
    Antagonist activity at EphA2 in human PC3 cells assessed as inhibition of ephrin-A1-Fc-stimulated EphA2 phosphorylation pretreated for 20 mins by sandwich ELISA
    Antagonist activity at EphA2 in human PC3 cells assessed as inhibition of ephrin-A1-Fc-stimulated EphA2 phosphorylation pretreated for 20 mins by sandwich ELISA
    [PMID: 23489211]
    RKO IC50
    > 200 μM
    Compound: LCA
    Anticancer activity against human RKO cells assessed as inhibition of cell proliferation by MTT assay
    Anticancer activity against human RKO cells assessed as inhibition of cell proliferation by MTT assay
    [PMID: 36439975]
    SK-HEP1 IC50
    > 200 μM
    Compound: LCA
    Anticancer activity against human SK-HEP1 cells assessed as inhibition of cell proliferation by MTT assay
    Anticancer activity against human SK-HEP1 cells assessed as inhibition of cell proliferation by MTT assay
    [PMID: 36439975]
    SW480 IC50
    > 200 μM
    Compound: LCA
    Anticancer activity against human SW480 cells assessed as inhibition of cell proliferation by MTT assay
    Anticancer activity against human SW480 cells assessed as inhibition of cell proliferation by MTT assay
    [PMID: 36439975]
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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.

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male mice (C57BL/6)[4].
    Dosage: 0.6% LCA-supplement diet, with the AIN93G diet as a control
    Administration: in diet, for 6 days
    Result: Induced liver injury.
    Activated TGFβ-SMAD3 signaling.
    Increased serum ALP activities.
    Animal Model: Male mice (C57BL/6)[2].
    Dosage: 125 mg/kg, dissolved in corn oil
    Administration: i.p., twice a day for four days
    Result: Induced liver injury, generated necrosis and neutrophilic-granulocytic infiltrate (H&E staining).
    Increased AST, ALT and ALP level.
    Molecular Weight

    376.57

    Formula

    C24H40O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCC(O)=O)([H])[C@@]3([H])[C@]([C@@]4([C@](C[C@H](O)CC4)([H])CC3)C)([H])CC1

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (265.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 10 mg/mL (26.56 mM; ultrasonic and warming and heat to 60°C)

    H2O : 0.99 mg/mL (2.63 mM; ultrasonic and warming and adjust pH to 11 with NaOH and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (5.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (5.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.96%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / Ethanol / DMSO 1 mM 2.6555 mL 13.2777 mL 26.5555 mL 66.3887 mL
    Ethanol / DMSO 5 mM 0.5311 mL 2.6555 mL 5.3111 mL 13.2777 mL
    10 mM 0.2656 mL 1.3278 mL 2.6555 mL 6.6389 mL
    15 mM 0.1770 mL 0.8852 mL 1.7704 mL 4.4259 mL
    20 mM 0.1328 mL 0.6639 mL 1.3278 mL 3.3194 mL
    25 mM 0.1062 mL 0.5311 mL 1.0622 mL 2.6555 mL
    DMSO 30 mM 0.0885 mL 0.4426 mL 0.8852 mL 2.2130 mL
    40 mM 0.0664 mL 0.3319 mL 0.6639 mL 1.6597 mL
    50 mM 0.0531 mL 0.2656 mL 0.5311 mL 1.3278 mL
    60 mM 0.0443 mL 0.2213 mL 0.4426 mL 1.1065 mL
    80 mM 0.0332 mL 0.1660 mL 0.3319 mL 0.8299 mL
    100 mM 0.0266 mL 0.1328 mL 0.2656 mL 0.6639 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Product Name:
    Lithocholic acid
    Cat. No.:
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