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Ezetimibe

现货
Catalog No.
A8430
胆固醇转运抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 800.00
现货
50mg
¥ 700.00
现货
100mg
¥ 1,000.00
现货

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Background

Ezetimibe is a potent and novel inhibitor of cholesterol absorption [1].

Cholesterol is a lipid molecule and is required to build and maintain membranes structural integrity and fluidity. Also, it serves as a precursor of vitamin D, bile acids and steroid hormones.

In differentiated Caco-2 cells incubated with a carotenoid (1 μM), ezetimibe (10 mg/L) inhibited carotenoid transport with 50% inhibition for ɑ-carotene and β-carotene. Also, it inhibited the transport of β-cryptoxanthin, lycopene and lutein:zeaxanthin(1:1). At the same time, ezetimibe inhibited cholesterol transport by 31%. Ezetimibe decreased the expression of the surface receptors SR-BI, ATP binding cassette transporter, subfamily A (ABCA1), Niemann-Pick type C1 Like 1 protein (NPC1L1) and retinoid acid receptor (RAR)γ, sterol-regulatory element binding proteins SREBP-1 and SREBP-2, and liver X receptor (LXR)β [3].

In apolipoprotein E knockout (apoE-/-) mice, ezetimibe (3 mg/kg) inhibited cholesterol absorption by 90%. Ezetimibe reduced plasma cholesterol, increased HDL levels, and inhibits the progression of atherosclerosis [1]. In phase III human trials, Ezetimibe (10 mg) significantly reduced the levels of LDL cholesterol, total cholesterol and triglycerides and increased the level of HDL cholesterol [2].

References:
[1].  Davis HR Jr, Compton DS, Hoos L, et al. Ezetimibe, a potent cholesterol absorption inhibitor, inhibits the development of atherosclerosis in ApoE knockout mice. Arterioscler Thromb Vasc Biol, 2001, 21(12): 2032-2038.
[2].  Clader JW. The discovery of ezetimibe: a view from outside the receptor. J Med Chem, 2004, 47(1): 1-9.
[3].  During A, Dawson HD, Harrison EH. Carotenoid transport is decreased and expression of the lipid transporters SR-BI, NPC1L1, and ABCA1 is downregulated in Caco-2 cells treated with ezetimibe. J Nutr, 2005, 135(10): 2305-2312.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt409.4
Cas No.163222-33-1
FormulaC24H21F2NO3
Solubility≥20.45mg/mL in DMSO
Chemical Name(3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
SDFDownload SDF
Canonical SMILESC1=CC(=CC=C1C2C(C(=O)N2C3=CC=C(C=C3)F)CCC(C4=CC=C(C=C4)F)O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

Caco-2细胞系

溶解方法

在DMSO中的溶解度> 20.5mg/mL。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

1-10 μg/mL

应用

在Caco-2细胞中,Ezetimibe是类胡萝卜素转运的抑制剂,活性随着类胡萝卜素分子极性的增加而减少。Ezetimibe不仅与胆固醇转运蛋白有物理相互作用,而且可以下调这些蛋白质的表达。

动物实验[2]:

动物模型

载脂蛋白E基因敲除(ApoE-/-)小鼠

剂量

5 mg/kg每天,持续6个月

应用

在(ApoE-/-)小鼠中,Ezetimibe可抑制胆固醇吸收,降低血浆胆固醇,增加高密度脂蛋白水平,并在低脂肪和无胆固醇饮食条件下抑制动脉粥样硬化的进展。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] During A, Dawson HD, Harrison EH. Carotenoid transport is decreased and expression of the lipid transporters SR-BI, NPC1L1, and ABCA1 is downregulated in Caco-2 cells treated with ezetimibe. J Nutr, 2005, 135(10): 2305-2312.

[2] Davis HR Jr, Compton DS, Hoos L, et al. Ezetimibe, a potent cholesterol absorption inhibitor, inhibits the development of atherosclerosis in ApoE knockout mice. Arterioscler Thromb Vasc Biol, 2001, 21(12): 2032-2038.

质量控制

化学结构

Ezetimibe