22(R)-Hydroxycholesterol
Based on 1 Customer Validation
22 (R)-Hydroxycholesterol (Narthesterol) is a natural oxysterol, acting as a LXRα agonist that inhibits cancer cell proliferation. 22 (R)-Hydroxycholesterol activates LXRα-mediated upregulation of downstream ABCA1 expression, enhances apolipoprotein-dependent cholesterol efflux, reduces intracellular cholesterol content, and decreases the production of β-amyloid peptide. 22 (R)-Hydroxycholesterol induces the differentiation of human mesenchymal stem cells into functional dopaminergic neurons. 22 (R)-Hydroxycholesterol is applicable to research related to cancer, Alzheimer's disease, and Parkinson's disease.
For research use only. We do not sell to patients.
- Purity : 99.86%
- CAS No.: 17954-98-2
- Formula: C27H46O2
- Molecular Weight:402.65
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Endogenous Metabolite Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
LXRα |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | EC50 |
7.0 μM
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Antiproliferative activity against human DU-145 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
Antiproliferative activity against human DU-145 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
|
20944148 |
| MCF7 | EC50 |
7.4 μM
|
Antiproliferative activity against human MCF-7 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
Antiproliferative activity against human MCF-7 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
|
20944148 |
| SAOS-2 | EC50 |
7.6 μM
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Antiproliferative activity against human Saos-2 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
Antiproliferative activity against human Saos-2 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
|
20944148 |
| HeLa | EC50 |
7.7 μM
|
Antiproliferative activity against human HeLa cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
Antiproliferative activity against human HeLa cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
|
20944148 |
| PC-3 | EC50 |
7.7 μM
|
Antiproliferative activity against human PC-3 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
Antiproliferative activity against human PC-3 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
|
20944148 |
| MDA-MB-435 | EC50 |
8.0 μM
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Antiproliferative activity against human MDA-MB-435 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
Antiproliferative activity against human MDA-MB-435 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
|
20944148 |
| NCI-H1299 | EC50 |
8.4 μM
|
Antiproliferative activity against human H1299 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
Antiproliferative activity against human H1299 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
|
20944148 |
| A-431 | EC50 |
8.6 μM
|
Antiproliferative activity against human A431 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
Antiproliferative activity against human A431 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
|
20944148 |
| HepG2 | EC50 |
10.1 μM
|
Antiproliferative activity against human HepG2 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
Antiproliferative activity against human HepG2 cancer cells assessed as reduction in relative DNA content measured via Hoechst 33258 fluorescence after 96 hrs incubation.
|
20944148 |
In Vitro
22 (R)-Hydroxycholesterol (22R) (10‑20 μM; 24 h) combined with 9‑cis‑Retinoic acid (HY-15128) upregulates ABCA1 expression, enhances cholesterol efflux, modulates APP processing, and diminishes Aβ secretion in H4APPsw and CHOAPPsw cells[1].
22 (R)-Hydroxycholesterol (22-HC) (2 μM; 14 days) induces the differentiation of human BM-MSCs, AD-MSCs and DP-MSCs into dopaminergic neurons. Among them, DP-MSCs show the highest differentiation efficiency (80.20% of MAP2-positive cells), with the most significant upregulation of dopaminergic markers and functional properties[2].
22 (R)-Hydroxycholesterol (30 nM-3 μM) activates LXRα in transfected HEK293 cells. Significant activation is observed at a concentration of 1 μM, and an even higher level of activation is detected at 3 μM[3].
22 (R)-Hydroxycholesterol (1-12 μM; 96 h) inhibits the proliferation of the human prostate cancer cell subline LNCaP in a dose-dependent manner, with an EC50 value ranging from 4.7 μM to 6.3 μM; it also inhibits the proliferation of various human cancer cell lines in a dose-dependent manner, with EC50 values ranging from 7.0 μM to 10.1 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human bone marrow-derived mesenchymal stem cells (BM-MSCs), adipose tissue-derived mesenchymal stem cells (AD-MSCs), dental pulp-derived mesenchymal stem cells (DP-MSCs)
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Concentration:2 μM
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Incubation Time:14 days
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Result:Induced dopaminergic neuronal differentiation of human BM-MSCs, AD-MSCs, and DP-MSCs, with DP-MSCs exhibiting the highest differentiation efficiency (80.20% MAP2-positive cells) and most robust upregulation of dopaminergic markers and functional traits.
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Cell Line:LNCaP human prostate cancer cell sublines (104-S, 104-R1, 104-R2, R1Ad, CDXR-3, IS-3)
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Concentration:1 μM, 2 μM, 4 μM, 8 μM, 12 μM
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Incubation Time:96 h
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Result:Dose-dependently suppressed the proliferation of all tested cell sublines.
Achieved half-maximal effective concentration (EC50) values for growth inhibition of 4.7 μM (104-R2), 5.2 μM (CDXR-3), 5.7 μM (104-S), 5.8 μM (104-R1), 5.9 μM (IS-3), and 6.3 μM (R1Ad).
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Cell Line:multiple human cancer cell lines (DU-145, SCC13, MCF-7, Saos-2, HeLa, PC-3, MDA-MB-435, H1299, A431, HepG2)
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Concentration:1 μM, 2 μM, 4 μM, 8 μM, 12 μM
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Incubation Time:96 h
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Result:Dose-dependently suppressed the proliferation of all tested cell lines, with greater suppression observed at 8 μM or higher concentrations.
Achieved half-maximal effective concentration (EC50) values for growth inhibition of 7.0 μM (DU-145), 7.2 μM (SCC13), 7.4 μM (MCF-7), 7.6 μM (Saos-2), 7.7 μM (HeLa), 7.7 μM (PC-3), 8.0 μM (MDA-MB-435), 8.4 μM (H1299), 8.6 μM (A431), and 10.1 μM (HepG2).
Chemical Information
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CAS No. 17954-98-2
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Appearance Solid
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Molecular Weight 402.65
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Formula C27H46O2
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Color White to off-white
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SMILES
O[C@@H](CC[C@@]12C)CC1=CC[C@@]3([C@@]2(CC[C@]4([C@]3(CC[C@]4([H])[C@H](C)[C@@H](CCC(C)C)O)[H])C)[H])[H]
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Synonyms
Narthesterol
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
Ethanol : ≥ 100 mg/mL (248.35 mM)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
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.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (287 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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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 |
|---|---|---|---|---|---|
| Ethanol | 1 mM | 2.4835 mL | 12.4177 mL | 24.8355 mL | 62.0887 mL |
| 5 mM | 0.4967 mL | 2.4835 mL | 4.9671 mL | 12.4177 mL | |
| 10 mM | 0.2484 mL | 1.2418 mL | 2.4835 mL | 6.2089 mL | |
| 15 mM | 0.1656 mL | 0.8278 mL | 1.6557 mL | 4.1392 mL | |
| 20 mM | 0.1242 mL | 0.6209 mL | 1.2418 mL | 3.1044 mL | |
| 25 mM | 0.0993 mL | 0.4967 mL | 0.9934 mL | 2.4835 mL | |
| 30 mM | 0.0828 mL | 0.4139 mL | 0.8278 mL | 2.0696 mL | |
| 40 mM | 0.0621 mL | 0.3104 mL | 0.6209 mL | 1.5522 mL | |
| 50 mM | 0.0497 mL | 0.2484 mL | 0.4967 mL | 1.2418 mL | |
| 60 mM | 0.0414 mL | 0.2070 mL | 0.4139 mL | 1.0348 mL | |
| 80 mM | 0.0310 mL | 0.1552 mL | 0.3104 mL | 0.7761 mL | |
| 100 mM | 0.0248 mL | 0.1242 mL | 0.2484 mL | 0.6209 mL |
Keywords
- 22(R)-Hydroxycholesterol
- 17954-98-2
- Narthesterol
- Endogenous Metabolite
- LXR
- Amyloid-β
- ATP-binding cassette (ABC) transporters
- Liver X receptor
- CHOAPPsw cells
- LXRα
- retinoic X receptor
- LNCaP human prostate cancer cell sublines
- H4APPsw cells
- ATP-binding cassette transporter A1
- human mesenchymal stem cells
- amyloid precursor protein
- HEK293 cells
- Inhibitor
- inhibitor
- inhibit