1. Metabolic Enzyme/Protease
  2. Endogenous Metabolite
  3. Cholesteryl sulfate sodium

Cholesteryl sulfate sodium is an orally available, NPC2-targeted cholesterol biosynthesis agonist. Cholesteryl sulfate sodium activates SREBP2 by competitively binding to NPC2, promoting cholesterol synthesis (EC50=50 μM). Cholesteryl sulfate sodium enhances the self-assembly ability of Mitoxantrone hydrochloride (HY-13502A), while repairing the intestinal mucosal barrier and inhibiting inflammation by regulating serine protease activity and PKCη signaling pathway. Cholesteryl sulfate sodium is a component of the platelet cell membrane and supports platelet adhesion. Cholesteryl sulfate sodium also regulates the activity of selective protein kinase C isoforms and modulates the specificity of PI3K, playing a role in keratinocyte differentiation.

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Cholesteryl sulfate sodium Chemical Structure

Cholesteryl sulfate sodium Chemical Structure

CAS No. : 2864-50-8

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Based on 1 publication(s) in Google Scholar

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Description

Cholesteryl sulfate sodium is an orally available, NPC2-targeted cholesterol biosynthesis agonist. Cholesteryl sulfate sodium activates SREBP2 by competitively binding to NPC2, promoting cholesterol synthesis (EC50=50 μM). Cholesteryl sulfate sodium enhances the self-assembly ability of Mitoxantrone hydrochloride (HY-13502A), while repairing the intestinal mucosal barrier and inhibiting inflammation by regulating serine protease activity and PKCη signaling pathway. Cholesteryl sulfate sodium is a component of the platelet cell membrane and supports platelet adhesion. Cholesteryl sulfate sodium also regulates the activity of selective protein kinase C isoforms and modulates the specificity of PI3K, playing a role in keratinocyte differentiation[1][2][3].

In Vitro

Membrane Stabilization: Cholesteryl sulfate (10-50 μM; 30 min-1 h) protects human erythrocytes from osmotic lysis by enhancing membrane rigidity, acting as a physiologic stabilizer1.
Platelet Function: Cholesteryl sulfate (1-10 μM; 10 min) potentiates ADP- and thrombin-induced platelet aggregation and serotonin secretion via calcium flux modulation1.
Enzyme Regulation: Cholesteryl sulfate (5-50 μM; 1-2 h) inhibits serine proteases (e.g., thrombin, plasmin) and activates protein kinase Cη (PKCη) in epidermal cells, regulating inflammation and barrier formation1,2.
Cholesterol Biosynthesis: Cholesteryl sulfate (50 μM; 24 h) upregulates genes (e.g., HMGCS1, FDFT1) involved in cholesterol biosynthesis in HT-29 cells by binding to NPC2 and activating SREBP22.
Cellular Uptake: Cholesteryl sulfate-based nanoparticles (0.025-5 μM; 2-4 h) significantly enhance mitoxantrone hydrochloride (MTO) accumulation in cancer cells (e.g., 4T1, CT26) compared to free MTO3.

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

In Vivo

Cholesteryl sulfate sodium (0.004% diet; oral; once daily, 6 days) antagonizes acute ulcerative colitis induced by DSS (HY-116282C) in male C57BL/6J mice, prevents weight loss, colon shortening and tissue damage, and reverses the exacerbated symptoms in Sult2b1△IEC mice[2].
Cholesteryl sulfate sodium (0.004% diet; oral; once daily, 33 days) improves survival and reduces inflammation in male C57BL/6J mice with chronic colitis induced by DSS[2].
Cholesteryl sulfate sodium (0.004% diet; oral; once daily, 42 days) alleviates spontaneous colitis caused by IL-10 deficiency in female IL-10-/- mice and reduces body weight loss and tissue damage[2].
Cholesteryl sulfate sodium (SCS) can synergize with Mitoxantrone hydrochloride (HY-13502A) to exert antitumor activity through a nano-delivery system[3].

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

Molecular Weight

488.70

Formula

C27H45NaO4S

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CC(C)CCC[C@@H](C)[C@@]1([H])CC[C@@]2([H])[C@]3([H])CC=C4C[C@@H](OS([O-])(=O)=O)CC[C@]4(C)[C@@]3([H])CC[C@@]21C.[Na+]

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (20.46 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)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0462 mL 10.2312 mL 20.4625 mL
5 mM 0.4092 mL 2.0462 mL 4.0925 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 (stored under nitrogen, away from moisture). 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)

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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: ≥ 2.5 mg/mL (5.12 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 DMSO 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% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.12 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 DMSO 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:

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

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

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 (stored under nitrogen, away from moisture). 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 1 mM 2.0462 mL 10.2312 mL 20.4625 mL 51.1561 mL
5 mM 0.4092 mL 2.0462 mL 4.0925 mL 10.2312 mL
10 mM 0.2046 mL 1.0231 mL 2.0462 mL 5.1156 mL
15 mM 0.1364 mL 0.6821 mL 1.3642 mL 3.4104 mL
20 mM 0.1023 mL 0.5116 mL 1.0231 mL 2.5578 mL
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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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Cholesteryl sulfate sodium
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HY-111355B
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