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/ LDL / Ezetimibe/依泽替米贝

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

货号：A124629 同义名： SCH 58235; Ezetrol

Ezetimibe是一种胆固醇吸收抑制剂，在联合他汀治疗时能降低低密度脂蛋白（LDL）胆固醇水平。它也是一种Niemann-Pick C1-like1（NPC1L1）抑制剂和Nrf2激活剂。

HazMat Fee +

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/依泽替米贝 化学结构 CAS号：163222-33-1
Ezetimibe/依泽替米贝 化学结构
CAS号：163222-33-1
Ezetimibe/依泽替米贝 3D分子结构
CAS号：163222-33-1
Ezetimibe/依泽替米贝 化学结构 CAS号：163222-33-1
Ezetimibe/依泽替米贝 3D分子结构 CAS号：163222-33-1
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Ezetimibe/依泽替米贝 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/依泽替米贝 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/依泽替米贝 细胞实验

Cell Line
Concentration Treated Time Description References
AS patient PBMCs 20 µM 1 day To investigate the effect of Ezetimibe on Th17 cell differentiation in AS patient PBMCs, results showed that Ezetimibe significantly reduced the number of Th17 cells. Front Immunol. 2022 Aug 17;13:922531.
Human primary lung fibroblasts (hLFs) 20 µM 24 hours Ezetimibe inhibited TGFβ1-induced myofibroblast differentiation, restored intracellular cholesterol distribution, and suppressed fibrotic gene expression through the mTORC1-autophagy axis. Eur Respir J. 2024 May 16;63(5):2300580.
Mouse primary lung fibroblasts (mLFs) 20 µM 24 hours Ezetimibe inhibited TGFβ1-induced myofibroblast differentiation, restored intracellular cholesterol distribution, and suppressed fibrotic gene expression through the mTORC1-autophagy axis. Eur Respir J. 2024 May 16;63(5):2300580.
Mouse spleen cells 10 and 20 µM 3 days To investigate the effect of Ezetimibe on immune cell differentiation, results showed that Ezetimibe increased the number of Treg cells and reduced the number of Th17 and Th1 cells. Front Immunol. 2022 Aug 17;13:922531.
Rat mesenteric artery smooth muscle cells 5–50 µM To explore the direct vascular effect of Ezetimibe on rat mesenteric arteries, it was found that Ezetimibe induced concentration-dependent vasodilation. Int J Mol Sci. 2023 Sep 12;24(18):13992.

Ezetimibe/依泽替米贝 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c background SKG mice Ankylosing spondylitis model mice Oral 10 mg/kg Once daily for 6 weeks To investigate the efficacy of Ezetimibe in ankylosing spondylitis model mice, results showed that Ezetimibe significantly inhibited joint inflammation and spinal bending, and reduced the expression of proinflammatory cytokines. Front Immunol. 2022 Aug 17;13:922531.
C57BL/6J mice Bleomycin-induced pulmonary fibrosis model Oral gavage 2 mg/kg Three times a week for 21 days Ezetimibe ameliorated bleomycin-induced pulmonary fibrosis by inhibiting mTORC1 activity and increasing autophagic flux, reducing collagen accumulation and improving respiratory function. Eur Respir J. 2024 May 16;63(5):2300580.

Ezetimibe/依泽替米贝 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/依泽替米贝 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/依泽替米贝 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/依泽替米贝 技术信息

CAS号163222-33-1
分子式C24H21F2NO3
分子量 409.43
SMILES Code O=C1N(C2=CC=C(F)C=C2)[C@H](C3=CC=C(O)C=C3)[C@H]1CC[C@@H](C4=CC=C(F)C=C4)O
MDL No. MFCD00937872
别名 SCH 58235; Ezetrol; Ezetimibe, Zetia, Ezetrol,
运输蓝冰
InChI Key OLNTVTPDXPETLC-XPWALMASSA-N
Pubchem ID 150311
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二

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/依泽替米贝 纯度/质量文件 | Ezetimibe/依泽替米贝 生物活性 | Ezetimibe/依泽替米贝 临床数据 | Ezetimibe/依泽替米贝 参考文献 | Ezetimibe/依泽替米贝 实验方案 | Ezetimibe/依泽替米贝 技术信息

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