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| Other Sizes |
| Targets |
Cholesteryl hemisuccinate targets cancer cells, exhibiting anticancer activity. It inhibits the growth of murine C1498 myeloid and L1210 lymphocytic leukemia cells when used at concentrations of 50 and 150 μM. It also has hepatoprotective activity, inhibiting acetaminophen-induced hepatotoxicity and preventing AAP-induced hepatic apoptosis and necrosis. Its mechanism may involve modulation of cell membrane properties and signaling pathways.
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| ln Vitro |
In vitro, Cholesteryl hemisuccinate demonstrates anticancer activity. It inhibits the growth of murine C1498 myeloid and L1210 lymphocytic leukemia cells at concentrations of 50 and 150 μM. Its activity is typically assessed in cell viability assays using cancer cell lines. It also exhibits hepatoprotective activity in vitro, protecting cells from acetaminophen-induced toxicity.
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| ln Vivo |
AAP-induced apoptosis (350–500 mg/kg; ip; single dose) in ICR mice (CD-1) is eliminated by cholesterol hemisuccinate (100 mg/kg; ip; single dose) Histological and biochemical detection of necrosis [1].
In vivo, Cholesteryl hemisuccinate has hepatoprotective activity. It inhibits acetaminophen-induced hepatotoxicity and prevents AAP-induced hepatic apoptosis and necrosis. Its anticancer activity has also been observed in vivo in murine models. As a pH-responsive lipid, it is used in drug delivery systems to enhance the bioavailability of poorly soluble drugs. |
| Enzyme Assay |
For non-cellular studies, Cholesteryl hemisuccinate's properties as a lipid are characterized. Its ability to form liposomes or other lipid-based structures is evaluated. Its pH-responsive behavior is assessed by measuring its ionization state at different pH values. Its interaction with other lipids and membrane components can be studied using biophysical techniques such as differential scanning calorimetry or fluorescence spectroscopy.
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| Cell Assay |
For in vitro cellular experiments, cancer cell lines such as C1498 or L1210 are cultured and treated with Cholesteryl hemisuccinate at various concentrations. Cell viability is assessed using MTT or similar assays to determine its antiproliferative effects. For hepatoprotective studies, cells are treated with acetaminophen in the presence or absence of the compound, and cell viability is measured.
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| Animal Protocol |
In vivo animal studies for Cholesteryl hemisuccinate are conducted in models of cancer or liver injury. In hepatoprotective studies, mice are treated with acetaminophen to induce liver injury, and the compound is administered to assess its protective effects. Liver enzymes and histopathology are evaluated. In cancer models, tumor growth is measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Cholesteryl hemisuccinate are not extensively detailed in the provided sources. It has a molecular weight of 486.74 and is a white to off-white solid. It has a density of 1.06 g/mL. As a cholesterol derivative, it is expected to be incorporated into lipid membranes and have a long circulation time. Comprehensive pharmacokinetic studies are needed to fully characterize its ADME properties.
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| Toxicity/Toxicokinetics |
The toxicity profile of Cholesteryl hemisuccinate is not explicitly detailed in the provided sources. As a cholesterol derivative, it is likely to be well-tolerated, but standard laboratory safety precautions should be followed when handling it. It is intended for research use only and is not for human therapeutic applications. Comprehensive toxicological studies are needed to fully evaluate its safety.
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| References |
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| Additional Infomation |
Cholesterol hemisuccinate is a dicarboxylic acid monoester formed by the condensation of the hydroxyl group of cholesterol with the carboxyl group of succinic acid. It is a commonly used detergent, frequently used in protein crystallography, protein biochemistry research, and pharmacology as a cholesterol substitute. It functions as a detergent. It is a cholesterol ester, a dicarboxylic acid monoester, and a hemisuccinate. Its function is related to cholesterol.
Cholesteryl hemisuccinate is an anionic cholesterol derivative with a molecular formula of C31H50O4 and a molecular weight of 486.74. It has anticancer activity and hepatoprotective effects. It is used as a pH-responsive lipid in drug delivery systems and as a cholesterol mimetic in structural biology. This research compound is for laboratory use only and has not been approved for clinical applications. |
| Molecular Formula |
C31H50O4
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|---|---|
| Molecular Weight |
486.73
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| Exact Mass |
486.37
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| CAS # |
1510-21-0
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| PubChem CID |
65082
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
586.0±43.0 °C at 760 mmHg
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| Melting Point |
178 °C
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| Flash Point |
179.6±21.7 °C
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| Vapour Pressure |
0.0±3.5 mmHg at 25°C
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| Index of Refraction |
1.529
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| LogP |
10.32
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
35
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| Complexity |
815
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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)OC(=O)CCC(=O)O)C)C
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| InChi Key |
WLNARFZDISHUGS-MIXBDBMTSA-N
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| InChi Code |
InChI=1S/C31H50O4/c1-20(2)7-6-8-21(3)25-11-12-26-24-10-9-22-19-23(35-29(34)14-13-28(32)33)15-17-30(22,4)27(24)16-18-31(25,26)5/h9,20-21,23-27H,6-8,10-19H2,1-5H3,(H,32,33)/t21-,23+,24+,25-,26+,27+,30+,31-/m1/s1
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| Chemical Name |
4-[[(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]oxy]-4-oxobutanoic acid
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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 |
| 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) |
Ethanol : 25 mg/mL (51.36 mM)
DMSO : 10 mg/mL (20.55 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.14 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (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 EtOH + stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0545 mL | 10.2726 mL | 20.5453 mL | |
| 5 mM | 0.4109 mL | 2.0545 mL | 4.1091 mL | |
| 10 mM | 0.2055 mL | 1.0273 mL | 2.0545 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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