2. Metabolic Enzyme/Protease
  3. Endogenous Metabolite
  4. Cholestenone

Cholestenone  (Synonyms: 4-Cholesten-3-one)

Cat. No.: HY-113365 Purity: 98.70%
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Cholestenone (4-cholesten-3-one) is an orally available antimicrobial agent that is metabolized primarily in the liver as an intermediate oxidation product of cholesterol. Cholestenone inhibits human dermal fibroblast migration and fights Helicobacter pylori infection in vitro and in mouse models by inhibiting cholesterol-α-D-glucopyranoside (CGL). Cholestenone also alleviates metabolic disorders caused by obesity in db/db mice.

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Cholestenone Chemical Structure

Cholestenone Chemical Structure

CAS No. : 601-57-0

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Based on 1 publication(s) in Google Scholar

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Cholestenone Related Antibodies

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Description

Cholestenone (4-cholesten-3-one) is an orally available antimicrobial agent that is metabolized primarily in the liver as an intermediate oxidation product of cholesterol. Cholestenone inhibits human dermal fibroblast migration and fights Helicobacter pylori infection in vitro and in mouse models by inhibiting cholesterol-α-D-glucopyranoside (CGL). Cholestenone also alleviates metabolic disorders caused by obesity in db/db mice[1][2][3][4].

IC50 & Target

Human Endogenous Metabolite

 

In Vitro

Cholestenone (4.7-150μM, 4 days) inhibits the growth of Helicobacter pylori in a dose-dependent manner[1].
Cholestenone (150 μM, 2 days) inhibits the expression of CGL in Helicobacter pylori[1].
Cholestenone affects the ordering ability of the remaining cholesterol, increases N-palmitoyl-sphingomyelin (PSM) in a short period of time, and increases the turnover rate of cholesterol after replacing 25% of cholesterol[2].
Cholestenone (treated with 10U/mL coase for 1 hour; treated with 0.5mM MBDC for 5 minutes) inhibits the migration of human dermal fibroblasts.

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

Cholestenone Related Antibodies

Cell Migration Assay [2]

Cell Line: HDFs
Concentration: 25% cholesterol consumption (Cholesterol oxidase (HY-P2848) (10 U/ml; 1 h), Methyl-β-cyclodextrin (HY-101461) (0.5 mM; 5 min))
Incubation Time: 0 and 22 h
Result: Reduced the amount of cell migration.

Cell Proliferation Assay[1]

Cell Line: Helicobacter pylori ATCC 43504; Helicobacter pylori 2460
Concentration: 4.7-150 μM
Incubation Time: 0, 1, 2, 3, 4 days
Result: Inhibited the growth of Helicobacter pylori in a dose-dependent manner.
In Vivo

Cholestenone (oral, 0.5% wt/wt, 4 weeks) inhibits Helicobacter pylori in mice[1].
Cholestenone (oral; 1 g, once every eight hours, 17 consecutive days for dog; 1% cholestenone, 10 and 16 days for chicken) reduces plasma cholesterol levels in dogs and chickens, but does not reduce total cholesterol levels[3].
Cholestenone (oral, 0.25% cholestenone, 4 weeks) can alleviate obesity-related metabolic disorders in db/db mice[4].

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

Animal Model: Infected 5-wk-old C57BL/6 mice with two doses of 3 × 107 H. pylori strain SS1[1]
Dosage: 0.5% wt/wt
Administration: Oral; 4 weeks
Result: Inhibited the number of Helicobacter pylori.
Animal Model: dog; chicken[3]
Dosage: 1 g, once every eight hours,17 consecutive days for dog; 1% cholestenone, 10 and 16 days for chicken
Administration: Oral
Result: Reduced plasma cholesterol, total cholesterol levels did not decrease.
Animal Model: Obese diabetic db/db mice[4]
Dosage: 0.25% cholestenone; 4 weeks
Administration: Oral
Result: Relieved hyperlipidemia, hepatic cholesterol accumulation, and hyperinsulinemia, insufficient to improve hepatic triglyceride accumulation or obesity.
Increased fecal free fatty acids and neutral steroids.
Decreased plasma desmosterol, but not liver.
Molecular Weight

384.64

Formula

C27H44O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)CCC[C@@H](C)[C@H]1CC[C@@]2([H])[C@]3([H])CCC4=CC(CC[C@]4(C)[C@@]3([H])CC[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: 

Ethanol : 50 mg/mL (129.99 mM; Need ultrasonic)

DMSO : 2 mg/mL (5.20 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5998 mL 12.9992 mL 25.9983 mL
5 mM 0.5200 mL 2.5998 mL 5.1997 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.

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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

×
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% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 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% EtOH    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.50 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 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

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: 98.70%

COA (249 KB) HNMR (249 KB) LCMS (100 KB)

Handling Instructions (2659 KB)
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
DMSO / Ethanol 1 mM 2.5998 mL 12.9992 mL 25.9983 mL 64.9958 mL
5 mM 0.5200 mL 2.5998 mL 5.1997 mL 12.9992 mL
Ethanol 10 mM 0.2600 mL 1.2999 mL 2.5998 mL 6.4996 mL
15 mM 0.1733 mL 0.8666 mL 1.7332 mL 4.3331 mL
20 mM 0.1300 mL 0.6500 mL 1.2999 mL 3.2498 mL
25 mM 0.1040 mL 0.5200 mL 1.0399 mL 2.5998 mL
30 mM 0.0867 mL 0.4333 mL 0.8666 mL 2.1665 mL
40 mM 0.0650 mL 0.3250 mL 0.6500 mL 1.6249 mL
50 mM 0.0520 mL 0.2600 mL 0.5200 mL 1.2999 mL
60 mM 0.0433 mL 0.2167 mL 0.4333 mL 1.0833 mL
80 mM 0.0325 mL 0.1625 mL 0.3250 mL 0.8124 mL
100 mM 0.0260 mL 0.1300 mL 0.2600 mL 0.6500 mL
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Cholestenone Related Classifications

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.

Keywords:

Cholestenone601-57-04-Cholesten-3-oneEndogenous MetaboliteAntibacterialCholesterolHuman dermal fibroblastsDiabetic miceInhibitorinhibitorinhibit

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