| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Cholesteryl sulfate targets multiple protein kinase C (PKC) isoforms, particularly PKCε, PKCη, and PKCzeta, activating them at concentrations of 5-50 microM. It also inhibits serine proteases (e.g., thrombin, plasmin) and regulates the specificity of PI3K, playing a role in keratinocyte differentiation and platelet adhesion.
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| ln Vitro |
In vitro, cholesteryl sulfate (5-50 microM; 1-2 hours) inhibits serine proteases (e.g., thrombin, plasmin) and activates PKCη in epidermal cells, regulating inflammation and barrier formation. It also supports platelet adhesion and regulates the activity of selective PKC isoforms. It induces keratinocyte differentiation.
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| ln Vivo |
In vivo, cholesteryl sulfate sodium is used to study its role in skin barrier function, platelet adhesion, and inflammation. It is a component of the platelet cell membrane and supports platelet adhesion. It is also being investigated for its role in fixing intestinal mucosal barriers and inhibiting inflammation.
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| Enzyme Assay |
Non-cell assays are performed using purified PKC enzymes and a kinase activity kit. Cholesteryl sulfate is incubated with purified PKCη or PKCzeta in the presence of phosphatidylserine, calcium, and a PKC substrate peptide (e.g., histone H1) with [gamma-32P]ATP. Activity is measured by scintillation counting or by fluorescence polarization if using a fluorescent substrate.
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| Cell Assay |
For cell studies, Cholesteryl sulfate sodium is typically dissolved in aqueous buffers and added to keratinocyte or platelet cultures (1-50 microM). In epidermal cells, it activates PKCη and regulates inflammation. In platelets, it supports adhesion and regulates signaling pathways. Marker gene expression for differentiation is measured by qPCR.
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| Animal Protocol |
In animal models, cholesteryl sulfate sodium is applied topically to mouse skin to study its role in barrier function and wound healing. It is also administered to mice on a high-fat diet to study its effects on cholesterol metabolism and atherosclerosis. It can be delivered intraperitoneally or as an oral supplement, though its oral bioavailability is low.
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| ADME/Pharmacokinetics |
Cholesteryl sulfate is synthesized from cholesterol by sulfotransferase SULT2B1b. It is present in plasma at concentrations of approximately 0.1-1 microM and binds extensively to serum albumin and lipoproteins. It has a long half-life (days) and is excreted in the feces. The sodium salt improves water solubility for in vitro use.
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| Toxicity/Toxicokinetics |
The compound is non-toxic at physiological concentrations. High concentrations may be cytotoxic to some cell types due to membrane disruption and detergent-like effects. The sodium salt is considered safe for topical use in cosmetic and pharmaceutical formulations. No significant systemic toxicity has been reported at research doses.
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| References | |
| Additional Infomation |
Cholesteryl sulfate sodium is used in dermatology research as a model for skin barrier function and in studies of keratinocyte differentiation. It is also used as an internal standard for cholesterol sulfate analysis by mass spectrometry, as a PKC activator in cell signaling studies, and for investigating the role of sulfated sterols in inflammation and coagulation. It is not an approved drug.
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| Molecular Formula |
C27H45NAO4S
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|---|---|
| Molecular Weight |
488.70
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| Exact Mass |
488.293
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| CAS # |
2864-50-8
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| PubChem CID |
23679068
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| Appearance |
White to yellow solid powder
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| Melting Point |
178-180°C
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| LogP |
7.954
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
819
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@H](CCCC(C)C)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC=C4[C@@]3(CC[C@@H](C4)OS(=O)(=O)[O-])C)C.[Na+]
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| InChi Key |
LMPVQXVJTZWENW-KPNWGBFJSA-M
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| InChi Code |
InChI=1S/C27H46O4S.Na/c1-18(2)7-6-8-19(3)23-11-12-24-22-10-9-20-17-21(31-32(28,29)30)13-15-26(20,4)25(22)14-16-27(23,24)5;/h9,18-19,21-25H,6-8,10-17H2,1-5H3,(H,28,29,30);/q;+1/p-1/t19-,21+,22+,23-,24+,25+,26+,27-;/m1./s1
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| Chemical Name |
sodium;[(3S,8S,9S,10R,13R,14S,17R)-10,13-dimethyl-17-[(2R)-6-methylheptan-2-yl]-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl] sulfate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~10 mg/mL (~20.46 mM )
H2O :< 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2046 mL | 1.0231 mL | 2.0462 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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