22(R)-hydroxy Cholesterol (Synonyms:22(R)-羟基胆固醇;Narthesterol)
目录号 : KCM12060 CAS No. : 17954-98-2 纯度 : ≥98%
The liver X receptors (LXRα and LXRβ) are nuclear hormone receptors whose native ligands are oxysterols. LXRs regulate the oxysterol-induced expression of cholesterol 7α-hydroxylase, the rate limiting enzyme of classic bile acid synthesis. 22(R)-hydroxy Cholesterol is an endogenous agonist for LXRs that activates LXRα with an EC value of 325 nM. 22(R)-hydroxy Cholesterol, acting through LXR heterodimerized with the retinoid X receptor, induces the expression of the ABCA1 reverse cholesterol transporter. This activity increases the efflux of cholesterol from enterocytes and thus inhibits the overall absorption of cholesterol. 22(R)-hydroxy Cholesterol can be used as a substrate to monitor cholesterol transport or as an endogenous positive control for testing LXR agonists which have potential as therapeutic agents for the treatment of atherosclerosis.
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生物活性

22(R)-hydroxy Cholesterol 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.

IC50&Target
LXRα
体外研究

22(R)-hydroxy Cholesterol (10-20 μM; 24 h) combined with 9-cis Retinoic acid can upregulate the expression of ABCA1, increase cholesterol efflux, regulate APP processing, and reduce A β secretion in H4APPsw and CHOAPPsw cells.

22(R)-hydroxy Cholesterol (22-HC) (2 μM; 14 days) can induce human BM MSCs, AD MSCs, and DP MSCs to differentiate into dopaminergic neurons. Among them, DP MSCs have the highest differentiation efficiency (MAP2 positive cells account for 80.20%), and the upregulation of dopaminergic markers and functional characteristics is the most significant.
22(R)-hydroxy Cholesterol (30 nM-3 μM) can activate LXR α in transfected HEK293 cells, with significant activation observed at a concentration of 1 μM and higher activation levels at a concentration of 3 μM.
22(R)-hydroxy Cholesterol (1-12 μM; 96 h) can dose dependently inhibit the proliferation of human prostate cancer cell line LNCaP, with EC50 values ranging from 4.7 μM to 6.3 μM; It can dose dependently inhibit the proliferation of various human cancer cell lines, with EC50 values ranging from 7.0 μM to 10.1 μM.

 

Cell Differentiation Assay

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)
Concentration: 2 μM
Incubation Time: 14 days
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.

Cell Proliferation Assay

Cell Line: LNCaP human prostate cancer cell sublines (104-S, 104-R1, 104-R2, R1Ad, CDXR-3, IS-3)
Concentration: 1 μM, 2 μM, 4 μM, 8 μM, 12 μM
Incubation Time: 96 hours
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).

Cell Proliferation Assay

Cell Line: multiple human cancer cell lines (DU-145, SCC13, MCF-7, Saos-2, HeLa, PC-3, MDA-MB-435, H1299, A431, HepG2)
Concentration: 1 μM, 2 μM, 4 μM, 8 μM, 12 μM
Incubation Time: 96 hours
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).
 
分子式
C27H46O2
分子量
402.65
CAS号
17954-98-2
中文名称
22(R)-羟基胆固醇
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro:

Ethanol : ≥ 100 mg/mL (248.35 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4835 mL 12.4177 mL 24.8355 mL
5 mM 0.4967 mL 2.4835 mL 4.9671 mL
10 mM 0.2484 mL 1.2418 mL 2.4835 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% EtOH → 90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.21 mM,饱和度未知) 的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL ⽟⽶油中,混合均匀。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
动物实验计算换算器
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系客服为您提供正确的澄清溶液配方)
+
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计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积:

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。