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依泽替米贝 /Ezetimibe {[allProObj[0].p_purity_real_show]}

货号：A124629 同义名： SCH 58235;Ezetrol

Ezetimibe is a cholesterol-absorption inhibitor, reduces levels of low-density lipoprotein (LDL) cholesterol when added to statin treatment. It's also a Niemann-Pick C1-like1 (NPC1L1) inhibitor and Nrf2 activator.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Ezetimibe 化学结构 CAS号：163222-33-1
Ezetimibe 化学结构
CAS号：163222-33-1
Ezetimibe 3D分子结构
CAS号：163222-33-1
Ezetimibe 化学结构 CAS号：163222-33-1
Ezetimibe 3D分子结构 CAS号：163222-33-1
规格 价格 会员价 库存 数量
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Ezetimibe 纯度/质量文件 产品仅供科研

货号：A124629 标准纯度： {[allProObj[0].p_purity_real_show]}
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Ezetimibe 生物活性

描述 Ezetimibe is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe activates Nrf2-Keap1 pathway which was dependent of autophagy adaptor protein p62, without causing cytotoxicity. Ezetimibe activates AMP-activated protein kinase (AMPK), which in turn phosphorylates p62 (p-S351) via their direct interaction. Correspondingly, Ezetimibe protected liver cells from saturated fatty acid-induced apoptotic cell death through p62-dependent Nrf2 activation[3]. 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. In addition, autophagy-related mRNA expression including ATG5, ATG6, and ATG7 and the protein level of microtubule-associated protein light chain 3 (LC3) were significantly increased in the liver in rats that received ezetimibe[4]. Ezetimibe and pitavastatin in combination induced higher PCSK9 levels than pitavastatin monotherapy or co-therapy with ezetimibe plus Xuezhikang[5]. Long-term application of ezetimibe significantly reduced the concentrations of vitamin D3-d3 in the serum and tissues of mice[6]. Ezetimibe alone played the same protection against a moderate atherosclerotic lesion as atorvastatin, which was associated with lowering serum cholesterol, decreasing circulating inflammatory cytokines, and inhibiting macrophage accumulation in the lesions[7].

Ezetimibe 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00101439 Hypercholesterolemia Phase 3 Completed - -
NCT00101439 - Completed - -
NCT00863265 - Completed - -

Ezetimibe 参考文献

[1]Clader JW. The discovery of ezetimibe: a view from outside the receptor. J Med Chem. 2004 Jan 1;47(1):1-9.

[2]van Heek M, Farley C, et al. Ezetimibe selectively inhibits intestinal cholesterol absorption in rodents in the presence and absence of exocrine pancreatic function. Br J Pharmacol. 2001 Sep;134(2):409-17.

[3]Lee DH, Han DH, Nam KT, Park JS, Kim SH, Lee M, Kim G, Min BS, Cha BS, Lee YS, Sung SH, Jeong H, Ji HW, Lee MJ, Lee JS, Lee HY, Chun Y, Kim J, Komatsu M, Lee YH, Bae SH. Ezetimibe, an NPC1L1 inhibitor, is a potent Nrf2 activator that protects mice from diet-induced nonalcoholic steatohepatitis. Free Radic Biol Med. 2016 Oct;99:520-532

[4]Chang E, Kim L, Park SE, Rhee EJ, Lee WY, Oh KW, Park SW, Park CY. Ezetimibe improves hepatic steatosis in relation to autophagy in obese and diabetic rats. World J Gastroenterol. 2015 Jul 7;21(25):7754-63

[5]Zhang Y, Liu J, Li S, Xu RX, Sun J, Li JJ. Impact of currently prescribed lipid-lowering drugs on plasma PCSK9 concentration: single or in combination study in rats. Lipids Health Dis. 2014 Feb 18;13:35

[6]Kiourtzidis M, Kühn J, Schutkowski A, Baur AC, Hirche F, Stangl GI. Inhibition of Niemann-Pick C1-like protein 1 by ezetimibe reduces uptake of deuterium-labeled vitamin D in mice. J Steroid Biochem Mol Biol. 2020 Mar;197:105504

[7]Tie C, Gao K, Zhang N, Zhang S, Shen J, Xie X, Wang JA. Ezetimibe Attenuates Atherosclerosis Associated with Lipid Reduction and Inflammation Inhibition. PLoS One. 2015 Nov 10;10(11):e0142430

Ezetimibe 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.42mL

4.88mL

2.44mL

Ezetimibe 技术信息

CAS号163222-33-1
分子式C24H21F2NO3
分子量 409.425
别名 SCH 58235;Ezetrol;Ezetimibe, Zetia, Ezetrol,
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 190 mg/mL(464.07 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear

PO 0.5% CMC-Na 32 mg/mL suspension

Tags: Ezetimibe | 163222-33-1 | SCH 58235 | SCH58235 | SCH-58235 | Cholesterol Absorption Inhibitor | NF-κB | Autophagy | Keap1-Nrf2 | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ezetimibe 纯度/质量文件 | Ezetimibe 生物活性 | Ezetimibe 临床数据 | Ezetimibe 参考文献 | Ezetimibe 实验方案 | Ezetimibe 技术信息

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