Glycocholic acid hydrate

Name: Glycocholic acid hydrate
Brand: MedChemExpress
SKU: HY-N1423B
Rating: 5.0 (3 reviews)

Cat. No.: HY-N1423B Purity: 97.0%: Data Sheet
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Glycocholic acid hydrate is a bile acid derivative. Glycocholic acid hydrate downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid hydrate inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid hydrate modulates related bile acid receptor signaling. Glycocholic acid hydrate suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid hydrate can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

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

CAS No. : 1192657-83-2

Size	Stock	Quantity
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Glycocholic acid hydrate:

Glycocholic acid In-stock

3 Publications Citing Use of MCE Glycocholic acid hydrate

RT-PCR

: Glycocholic acid hydrate 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.

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Caspase 3

Caspase-9

Bax

Bcl-2

S1PR2

In Vitro

Glycocholic acid (0-500 μM; 0, 24, 48, 72 h) hydrate reduces the viability of human colon adenocarcinoma Caco-2 cells in a time- and concentration-dependent manner^[1].
Glycocholic acid (250 μM; 72 h) hydrate 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) hydrate 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) hydrate reduces hMDR1 promoter activity in human colon adenocarcinoma Caco-2 cells^[1].
Glycocholic acid (250 μM; 72 h) hydrate induces chromatin condensation, a marker of apoptosis, in human colon adenocarcinoma Caco-2 cells^[1].
Glycocholic acid (250 μM; 72 h) hydrate 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) hydrate modulates bile acid receptor gene expression in SNU-245 cholangiocarcinoma cells, reducing FXR expression and increasing TGR5 and S1PR2 expression^[2].
Glycocholic acid hydrate 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 hydrate 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) hydrate 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) hydrate significantly reduces E. coli K1037 motility on soft LB agar by downregulating fliC gene expression^[3].
Glycocholic acid (0.125-2%) hydrate 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.

Cell Viability Assay^[1]

Cell Line:	human colon adenocarcinoma Caco-2 cells
Concentration:	0 μM, 100 μM, 250 μM, 300 μM, 400 μM, 500 μM
Incubation Time:	0 h, 24 h, 48 h, 72 h
Result:	Reduced cell viability in a time-dependent manner, with the most profound effects seen after 72 h. Decreased cell viability to 80% after 72 h incubation with 250 μM. Caused further significant decreases in viability after 72 h at concentrations of 300, 400, 500 μM compared to lower concentrations. Maintained cell viability at 96% and 90% after 24 h and 48 h incubation with 250 μM, respectively.

Cell Viability Assay^[1]

Cell Line:	human colon adenocarcinoma Caco-2 cells
Concentration:	250 μM (in combination with Epirubicin (HY-13624))
Incubation Time:	72 h
Result:	Reduced the mean IC₅₀ value of epirubicin to 8.08 μg/mL, which was significantly lower than the IC₅₀ value for epirubicin alone.

RT-PCR^[1]

Cell Line:	human colon adenocarcinoma Caco-2 cells
Concentration:	250 μM
Incubation Time:	72 h
Result:	Significantly downregulated mRNA expression of MDR1 (P-gp), MRP1, MRP2, and Bcl-2. Significantly upregulated mRNA expression of Bax, caspase-3, caspase-9, and p53 compared to untreated controls. Significantly increased the Bax-to-Bcl-2 ratio. Showed no significant effect on caspase-8 expression.

Apoptosis Analysis^[1]

Cell Line:	human colon adenocarcinoma Caco-2 cells
Concentration:	250 μM
Incubation Time:	72 h
Result:	Increased the percentage of cells in the sub-G1 phase (apoptotic cells) to 26.8% after treatment, which was significantly higher than the control (1.3%) and epirubicin alone (20.6%).

Real Time qPCR^[2]

Cell Line:	SNU-245 cholangiocarcinoma (CCA) cell line
Concentration:	1.6 μM
Incubation Time:	48 h
Result:	Reduced FXR gene expression to 0.17-fold of untreated control levels. Increased TGR5 gene expression to 8.55-fold of untreated control levels, which was significantly higher than both control and taurochenodeoxycholic acid-treated cells. Increased S1PR2 gene expression to 3.4-fold of untreated control levels and 3.9-fold of taurochenodeoxycholic acid-treated cell levels.

Formula

C₂₆H₄₃NO₆.xH₂O

CAS No.

1192657-83-2

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.[x H2O]

Structure Classification

Steroids

Initial Source

Endogenous metabolite

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

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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; 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; 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL; 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.

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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).

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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: 97.0%

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Data Sheet (284 KB) SDS (252 KB)

COA (251 KB) HNMR (287 KB)

Handling Instructions (2659 KB)

References

[1]. Lo YL, et al. Inhibit multidrug resistance and induce apoptosis by using glycocholic acid and epirubicin. Eur J Pharm Sci. 2008;35(1-2):52-67. [Content Brief]

[2]. Song WS, et al. Discovery of glycocholic acid and taurochenodeoxycholic acid as phenotypic biomarkers in cholangiocarcinoma. Sci Rep. 2018;8(1):11088. Published 2018 Jul 23. [Content Brief]

[3]. Piscon B, et al. The Effect of glycocholic acid on the growth, membrane permeability, conjugation and antibiotic susceptibility of Enterobacteriaceae. Front Cell Infect Microbiol. 2025;15:1550545. Published 2025 Mar 20. [Content Brief]