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> Cholesterol [57-88-5]

Cholesterol [57-88-5]

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Katalog-Nummer HY-N0322-1g

Size : 1g

Marke : MedChemExpress


Beschreibung

Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins[1][2]. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist[3].

IC50 & Target

Microbial Metabolite

 

Human Endogenous Metabolite

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 20 μM
Compound: b1
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 30822712]
BJ IC50
> 50 μM
Compound: Cholesterol
Cytotoxicity against human BJ cells after 72 hrs by calcein AM assay
Cytotoxicity against human BJ cells after 72 hrs by calcein AM assay
[PMID: 22417637]
CCRF-CEM IC50
> 50 μM
Compound: Cholesterol
Cytotoxicity against human CEM cells after 72 hrs by calcein AM assay
Cytotoxicity against human CEM cells after 72 hrs by calcein AM assay
[PMID: 22417637]
HL-60 IC50
> 20 μM
Compound: b1
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 30822712]
HT-29 IC50
> 50 μM
Compound: 1
Cytotoxicity against human HT-29 cells after 48 hrs by Alamar Blue assay
Cytotoxicity against human HT-29 cells after 48 hrs by Alamar Blue assay
[PMID: 19473028]
HeLa IC50
> 50 μM
Compound: Cholesterol
Cytotoxicity against human HeLa cells after 72 hrs by calcein AM assay
Cytotoxicity against human HeLa cells after 72 hrs by calcein AM assay
[PMID: 22417637]
MCF7 IC50
> 20 μM
Compound: b1
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 30822712]
MCF7 IC50
> 50 μM
Compound: Cholesterol
Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM assay
Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM assay
[PMID: 22417637]
SMMC-7721 IC50
> 20 μM
Compound: b1
Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 30822712]
SW480 IC50
> 20 μM
Compound: b1
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 30822712]
Vero IC50
> 128 μg/mL
Compound: 6
Cytotoxicity against african green monkey Vero cells
Cytotoxicity against african green monkey Vero cells
[PMID: 18818073]
In Vitro

GT1-7 hypothalamic cells subjected to Cholesterol depletion in vitro produced 20-31% reductions in cellular Cholesterol content. All Cholesterol-depleted neuron-derived cells, exhibit decreased phosphorylation/activation of IRS-1 and AKT following stimulation by insulin, insulin-like growth factor-1, or the neurotrophins (NGF and BDNF). Reduction in cellular Cholesterol also results in increased basal autophagy and impairment of induction of autophagy by glucose deprivation[1].

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

Cholesterol Related Antibodies
In Vivo

Cholesterol can be used to create models of hyperlipidemia and atherosclerosis. The metabolic half-life of Cholesterol varies from a few hours to several years, depending on its association with different lipoproteins and the specific tissues in which it is located[4].

Induction of Hyperlipidemia[5][6]
Background
Hyperlipidemia is a group of disorders characterized by elevated concentrations of circulating lipids, including cholesterol, cholesterol esters, phospholipids and triglycerides. If the intake of cholesterol is too much, and exceeds the body's metabolic capacity, it may lead to increased plasma cholesterol levels, causing hyperlipidemia.
Specific Modeling Methods
Rat: Wistar • male • 18-week-old (period: 8 weeks)
Administration: 2% cholesterol; diet • 8 weeks
Note
(1) Rats were housed in a room maintained at a 12-h light-dark cycle and a constant temperature of 22±2 °C
(2) Wistar rats were always chosen for hyperlipidemia studies since this species shows a moderate increase in serum cholesterol and triglyceride level due to a high-cholesterol diet and no substantial atherosclerosis develops; therefore, the direct myocardial effect of hyperlipidemia, independent from atherosclerosis, can be studied in this model.
Modeling Indicators
Molecular changes: Significant increase in total cholesterol levels in blood samples (about 20%)
Correlated Product(s): /
Opposite Product(s): /

Induction of atherosclerosis[7][8]
Background
High levels of cholesterol in the blood, especially low-density lipoprotein cholesterol (LDL-C), can accumulate plaque on the walls of blood vessels, a process known as atherosclerosis. Over time, these plaques can block blood flow and cause serious health problems such as myocardial ischemia or myocardial infarction.
Specific Modeling Methods
Rabbits: Oryctolagus cuniculus • male • 4-6-month-old (period: 16 weeks)
Administration: 0.3% cholesterol and 3% soybean oil; diet • 16 weeks
Note
(1) The cholesterol-fed rabbit is a widely used model for experimental atherosclerosis research as cholesterol only cause atherosclerotic changes in the rabbit arterial intima, which was very similar to human atherosclerosis.
(2) As the absorption of dietary cholesterol requires fat, you must add oil into the diet. Otherwise, rabbits will use their internal fat, which makes them lean or sick. In addition, using soybean oil, which consists of unsaturated fatty acids, can prevent the levels of plasma cholesterol from becoming too high. Other vegetable oils, such as peanut oil or corn oil, can be used because they are all unsaturated fatty acids. Animal fat (saturated fatty acids) like tallow and lard is not recommended.
(3) 0.3-0.5% cholesterol diet is recommended for most experiments. Rabbits cannot tolerate a 1-2% cholesterol diet for a month as they develop severe liver dysfunction.
(4) Adult rabbits at 4 months or older can consume approximately ~150 g a day. You can either feed ab libitum or restricted (100-150 g/day/adult rabbit).
(5) Plasma lipids should be measured weekly, especially for the first 4 weeks, because you need to determine whether plasma levels of cholesterol are elevated in each animal. Non-responder rabbits can be excluded from the experiments if their plasma cholesterol levels do not increase after cholesterol diet feeding.
(6) Plasma lipoproteins can be measured at 8 and 16 weeks when the plasma levels of cholesterol are stable.
(7) The age of rabbits should be considered because young rabbits are more susceptible to aortic atherosclerosis than old rabbits even though they have similar plasma cholesterol levels. 4-6-month-old rabbits are usually used for cholesterol feeding experiments.
(8) Male and female rabbits are different in terms of response to a cholesterol diet and atherosclerosis. In our experience, female rabbits develop higher hypercholesterolemia and greater aortic lesions than their counterpart male rabbits. In general, male rabbits are recommended for experiments because estrogen may influence the results.
Modeling Indicators
Histological changes: atherosclerosis lesions can be seen on HE stained aortic arch and thoracic aorta segments
Correlated Product(s): Soybean oil (HY-108750)
Opposite Product(s): /

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

386.65

Formel

C27H46O
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H](C1)CC[C@@]2(C)C1=CC[C@]3(17)[C@]2(17)CC[C@@]4(C)[C@@]3(17)CC[C@]4(17)[C@@H](CCCC(C)C)C
Structure Classification
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

Ethanol : 10 mg/mL (25.86 mM; ultrasonic and warming and heat to 60°C)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5863 mL 12.9316 mL 25.8632 mL
5 mM 0.5173 mL 2.5863 mL 5.1726 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.

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: ≥ 1.43 mg/mL (3.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (14.3 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% Corn Oil

    Solubility: ≥ 1.43 mg/mL (3.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 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 EtOH stock solution (14.3 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.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
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