1. GPCR/G Protein Apoptosis Membrane Transporter/Ion Channel Anti-infection Metabolic Enzyme/Protease
  2. Bacterial Bcl-2 Family LPL Receptor FXR P-glycoprotein MDM-2/p53 Caspase Apoptosis G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite
  3. Glycocholic acid

Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

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

CAS No. : 475-31-0

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10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Glycocholic acid:

Top Publications Citing Use of Products

    Glycocholic 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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA)[1][2][3].

    IC50 & Target[1]

    Microbial Metabolite

     

    Human Endogenous Metabolite

     

    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    13.6 μM
    Compound: 5b, glyco
    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]
    HEK293 IC50
    400 μM
    Compound: Glycocholate
    TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing HEK-293 cells
    TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing HEK-293 cells
    [PMID: 12523936]
    In Vitro

    Glycocholic acid (0-500 μM; 0, 24, 48, 72 h) reduces the viability of human colon adenocarcinoma Caco-2 cells in a time- and concentration-dependent manner[1].
    Glycocholic acid (250 μM; 72 h) at 250 μM significantly increases the chemosensitivity of human colon adenocarcinoma Caco-2 cells to Epirubicin (HY-13624)[1].
    Glycocholic acid (250 μM; 72 h) alters the expression of multidrug resistance and apoptosis-related genes in human colon adenocarcinoma Caco-2 cells, downregulating MDR1, MRP1, MRP2, and Bcl-2 while upregulating Bax, caspase-3, caspase-9, and p53, and increasing the Bax-to-Bcl-2 ratio[1].
    Glycocholic acid (250 μM; 72 h) reduces hMDR1 promoter activity in human colon adenocarcinoma Caco-2 cells[1].
    Glycocholic acid (250 μM; 72 h) induces chromatin condensation, a marker of apoptosis, in human colon adenocarcinoma Caco-2 cells[1].
    Glycocholic acid (250 μM; 72 h) increases the sub-G1 DNA content population, indicating apoptosis, in human colon adenocarcinoma Caco-2 cells[1].
    Glycocholic acid (GCA) (1.6 μM; 48 h) modulates bile acid receptor gene expression in SNU-245 cholangiocarcinoma cells, reducing FXR expression and increasing TGR5 and S1PR2 expression[2].
    Glycocholic acid inhibits late logarithmic phase growth of E. coli K1037, clinical UTI E. coli, Klebsiella pneumoniae, Klebsiella oxytoca, Salmonella Typhimurium, Raoultella ornithinolytica, and Citrobacter freundii in liquid LB culture, but not on solid LB agar medium[3].
    Glycocholic acid reduces the MIC of ampicillin for E. coli K1037 by 2-fold and the MIC of chloramphenicol for Raoultella ornithinolytica and Citrobacter freundii by 2-fold, resulting in additive antimicrobial interactions (FIC index 0.625-0.75)[3].
    Glycocholic acid (0.125-2%; 6 h) reduces conjugation frequency of multiple Enterobacteriaceae conjugative plasmids by 70 to 97% in a dose-dependent manner, with no prominent reduction in donor strain viability[3].
    Glycocholic acid (0.2-2%; 16 h) significantly reduces E. coli K1037 motility on soft LB agar by downregulating fliC gene expression[3].
    Glycocholic acid (0.125-2%) increases membrane permeability and compromises membrane integrity of E. coli K1037, as shown by increased NPN/EtBr uptake and cytoplasmic DnaK leakage[3].

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

    Clinical Trial
    Molecular Weight

    465.62

    Formula

    C26H43NO6

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)CNC(CC[C@@H](C)[C@H]1CC[C@@]2([H])[C@]3([H])[C@H](O)C[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])C[C@H](O)[C@]12C)=O

    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: 

    Methanol : ≥ 100 mg/mL (214.77 mM)

    DMSO : ≥ 100 mg/mL (214.77 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1477 mL 10.7384 mL 21.4767 mL
    5 mM 0.4295 mL 2.1477 mL 4.2953 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.47 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (4.47 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    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: 99.90%

    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
    Methanol / DMSO 1 mM 2.1477 mL 10.7384 mL 21.4767 mL 53.6919 mL
    5 mM 0.4295 mL 2.1477 mL 4.2953 mL 10.7384 mL
    10 mM 0.2148 mL 1.0738 mL 2.1477 mL 5.3692 mL
    15 mM 0.1432 mL 0.7159 mL 1.4318 mL 3.5795 mL
    20 mM 0.1074 mL 0.5369 mL 1.0738 mL 2.6846 mL
    25 mM 0.0859 mL 0.4295 mL 0.8591 mL 2.1477 mL
    30 mM 0.0716 mL 0.3579 mL 0.7159 mL 1.7897 mL
    40 mM 0.0537 mL 0.2685 mL 0.5369 mL 1.3423 mL
    50 mM 0.0430 mL 0.2148 mL 0.4295 mL 1.0738 mL
    60 mM 0.0358 mL 0.1790 mL 0.3579 mL 0.8949 mL
    80 mM 0.0268 mL 0.1342 mL 0.2685 mL 0.6711 mL
    100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5369 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Glycocholic acid
    Cat. No.:
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