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  4. Lithocholic acid

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

Cat. No.: HY-B0172 Purity: ≥98.0%
COA Handling Instructions

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.

Lithocholic acid Chemical Structure

Lithocholic acid Chemical Structure

CAS No. : 434-13-9

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 33 In-stock
Solution
10 mM * 1 mL in DMSO USD 33 In-stock
Solid
500 mg USD 30 In-stock
1 g USD 42 In-stock
5 g USD 75 In-stock
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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Lithocholic acid:

Top Publications Citing Use of Products
  • 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

 

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

Lithocholic acid (0.6% in supplement diet, 7 days) increases TGFB1, TGFBR1, and TGFBR2 mRNA levels in the liver of male mice (C57BL/6), and activates SMAD3, and induces biliary injury[4].
Lithocholic acid (125 mg/kg, i.p., twice a day for four days) induces liver damage, and increased AST, ALT and ALP level in male C57BL/6 mice[2].

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 : 250 mg/mL (663.89 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
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Concentration
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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

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Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥98.0%

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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Help & FAQs
  • Do most proteins show cross-species activity?

    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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Lithocholic acid
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