1. NF-κB
    Autophagy
  2. Keap1-Nrf2
    Autophagy
  3. Ezetimibe

Ezetimibe (Synonyms: 依泽替米贝; SCH 58235)

目录号: HY-17376 纯度: 99.93%
产品使用指南

Ezetimibe (SCH 58235) 是有效的胆固醇吸收 (cholesterol-absorption) 抑制剂。Ezetimibe 是一种 NPC1L1 抑制剂,是有效的 Nrf2 激活剂。

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Ezetimibe Chemical Structure

Ezetimibe Chemical Structure

CAS No. : 163222-33-1

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规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥500 In-stock
10 mg ¥400 In-stock
50 mg ¥714 In-stock
100 mg ¥1000 In-stock
200 mg ¥1500 In-stock
500 mg ¥3000 In-stock
1 g   询价  
5 g   询价  

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.

IC50 & Target

NPC1L1, Nrf2[1]

体外研究
(In Vitro)

Ezetimibe (Eze) acts as a potent Nrf2 activator without causing cytotoxicity. Ezetimibe enhances transactivation of Nrf2, as revealed by a luciferase reporter assay. Ezetimibe also upregulates Nrf2 target genes, including GSTA1, heme oxygenase-1 (HO-1) and Nqo-1 in Hepa1c1c7 and MEF cells. Ezetimibe upregulates Nrf2 target genes in Nrf2+/+ MEF cells, whereas this induction is totally blocked in Nrf2-/- MEF cells. Taken together, Ezetimibe acts as a novel Nrf2 inducer in a ROS-independent manner[1]. Human huh7 hepatocytes are pretreated with Ezetimibe (10 μM, 1 h) and incubated with palmitic acid (PA, 0.5 mM, 24 h) to induce hepatic steatosis. Ezetimibe treatment significantly attenuates PA-increased triglycerides (TG) levels, which is consistent with our animal study. PA treatment resulted in an approximately 20% decrease in mRNA expression of ATG5, ATG6, and ATG7, which had been increased by Ezetimibe treatment. In addition, Ezetimibe treatment significantly increased the PA-induced reduction in LC3 protein abundance[2].

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

体内研究
(In Vivo)

Administration of Ezetimibe (Eze) reduces the liver weights of mice fed the methionine- and choline-deficient (MCD) diet. This is consistent with the beneficial effects of Ezetimibe on hepatic steatosis. Liver histology shows pronounced multiple macrovesicular fat droplets in mice on the MCD diet, but Ezetimibe treatment markedly decreases the number and size of those droplets. Furthermore, hepatic fibrosis in mice fed the MCD diet is significantly attenuated by Ezetimibe[1]. Blood and liver lipid levels including TG, free fatty acids (FFA), and total cholesterol (TC) are significantly decreased in Ezetimibe-treated OLETF rats. Moreover, OLETF rats show higher serum levels of glucose, insulin, HOMA-IR, TG, FFA, and TC than LETF animals, which are significantly reduced by Ezetimibe. In addition, histological analysis indicated that OLETF control rats showed larger lipid droplets in hepatocytes than age-matched LETO controls, which are attenuated by administration of Ezetimibe[2].

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

Clinical Trial
分子量

409.43

Formula

C₂₄H₂₁F₂NO₃

CAS 号
中文名称

依泽替米贝

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (244.24 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 2.4424 mL 12.2121 mL 24.4242 mL
5 mM 0.4885 mL 2.4424 mL 4.8848 mL
10 mM 0.2442 mL 1.2212 mL 2.4424 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。-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% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.11 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.11 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 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Kinase Assay
[1]

GST-p62 is prepared from Escherichia coli and 0.5 μg of the purified GST-p62 protein is used for in vitro AMPK phosphorylation assay. Phosphorylation of p62 protein by AMPK is determined by non-radioisotope method using γS-ATP. AMPK complex is immuno-purified from the HEK293 cells, to which either myc-AMPKα1 wild-type (WT) or myc-AMPKα1 kinase-dead mutant (KD, D157A) is transfected with Flag-AMPKβ1 and HA-AMPKγ1. AMPK complex is added into the reaction mixture containing 20 mM HEPES, pH7.4, 1 mM EGTA, 0.4 mM EDTA, 5 mM MgCl2, 0.05 mM DTT, 0.5 μg GST-p62, 0.2 mM AMP, and 1 mM ATPγS. Reaction is carried out at 37°C for 30 min, and then terminated by adding 20 mM EDTA. To detect γS-labeled p62 protein, the reaction product is alkylated with 2.5 mM PNBM for 2 h at room temperature and analyzed the products by western blotting using anti-thiophosphate antibody[1].

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

Cell Assay
[2]

Huh7 human hepatocytes are cultured in high glucose DMEM containing 10% FBS, 100 units/mL penicillin and 100 μg/mL streptomycin at 37°C in a 95% air/5% CO2 atmosphere. Hepatocytes are treated with or without Ezetimibe (10 μM, 1 h) and incubated with palmitic acid (PA, 0.5 mM, 24 h)[2].

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

Animal Administration
[1][2]

Mice[1]
Ten-week-old C57BL/6J male mice are used. These animals are randomly assigned to one of three groups (7-10 mice in each group): normal chow diet; MCD diet, vehicle-treated; or MCD diet, Ezetimibe -treated. The mice had free access to diet and water, with temperature maintained at 23±2°C, humidity of 60%±10%, and 12-h light/dark cycles. In the MCD diet with Ezetimibe group, Ezetimibe 10 mg/kg is given once daily by oral gavage for 4 weeks. The chow and MCD diet with vehicle groups received the same volume of phosphate buffered saline orally for 4 weeks. Body weight is measured once a week over the course of the treatment period. After 4 weeks, the mice are anesthetized and killed; blood is collected via heart puncture. Tissues are harvested and either snap-frozen in liquid nitrogen and stored at −70°C or fixed in formalin and embedded in paraffin.
Rats[2]
Male OLETF (n=11) and age-matched LETO rats (n=3) are used, and experiments are conducted in a specific pathogen-free facility with a 12 h light/dark cycle. The OLETF rat is a model that represents late-onset hyperglycemia and exhibits a chronic disease course, mild obesity and clinical onset of diabetes mellitus. Animals have unrestricted access to water and food. At 12 wk of age, rats are randomized and treated with either PBS or Ezetimibe (10 mg/kg per day) via a stomach gavage for 20 wk. At the end of the study, the rats are fasted overnight and anesthetized with intraperitoneal Zoletil/Rompun. Blood is collected from the abdominal aorta, and liver tissues are dissected, immediately frozen in liquid nitrogen, and stored at -80°C until further analysis.

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

参考文献

Purity: 99.93%

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