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Etomoxir (Synonyms: (R)-(+)-Etomoxir)

目录号: HY-50202 纯度: 99.65%
产品使用指南

Etomoxir ((R)-(+)-Etomoxir) 是肉碱棕榈酰转移酶 1a (CPT-1a) 抑制剂,通过抑制 CPT-1a 可抑制脂肪酸氧化,并抑制人、大鼠和豚鼠中棕榈酸酯的氧化。

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Etomoxir Chemical Structure

Etomoxir Chemical Structure

CAS No. : 124083-20-1

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

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 ¥880 In-stock
5 mg ¥800 In-stock
10 mg ¥1500 In-stock
50 mg ¥5300 In-stock
100 mg   询价  
200 mg   询价  

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Top Publications Citing Use of Products

    Etomoxir purchased from MCE. Usage Cited in: Oncotarget. 2016 Oct 11;7(41):67071-67086.

    MDA-MB-453 cells are treated as indicated for 2 days and subjected to immunoblotting. Combination treatments using non-saturating doses of Etomoxir and MTI-31 or Rapamycin results in an enhanced growth suppression in MDA-MB-453 cells, which is not readily observed in MDA-MB-231 cells, correlating a nearly complete suppression of cyclin D1 and c-Myc level in MDA-MB-453 cells under the combination treatments.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.

    IC50 & Target

    CPT-1a[5]

    体外研究
    (In Vitro)

    Etomoxir binds irreversibly to the catalytic site of CPT-1 inhibiting its activity, but also upregulates fatty acid oxidation enzymes. Etomoxir is developed as an inhibitor of the mitochondrial carnitine palmitoyltransferase-1 (CPT-1) located on the outer mitochondrial membrane. Etomoxir, in the liver can act as peroxisomal proliferator, increasing DNA synthesis and liver growth. Thus, etomoxir, in addition of being a CPT1 inhibitor could be considered as a PPARalpha agonist[1]. Etomoxir is a member of the oxirane carboxylic acid carnitine palmitoyl transferase I inhibitors and has been suggested as a therapeutic agent for the treatment of heart failure. Acute Etomoxir treatment irreversibly inhibits the activity of carnitine palmitoyltransferase I. As a result, fatty acid import into the mitochondria and β-oxidation is reduced, whereas cytosolic fatty acid accumulates and glucose oxidation is elevated. Prolonged incubation (24 h) with Etomoxir produces diverse effects on the expression of several metabolic enzyme[2].

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

    体内研究
    (In Vivo)

    Etomoxir is an inhibitor of free fatty acid (FFA) oxidation-related key enzyme CPT1. P53 interacts directly with Bax, which is inhibited by Etomoxir, further confirming the direct interaction of P53 and Bax, and the involvement of FAO-mediated mitochondrial ROS generation in db/db mice[3]. Rats are injected daily with Etomoxir, a specific CPT-I inhibitor, for 8 days at 20 mg/kg of body mass. Etomoxir-treated rats display a 44% reduced cardiac CPT-I activity. The treatment of Lewis rats for 8 days with 20 mg/kg Etomoxir does not alter blood glucose, which is in line with comparable etomoxir-feeding studies. Similarly, Etomoxir feeding does not affect general growth characteristics such as gain in body mass, nor does it affect hindlimb muscle mass. However, heart mass and liver mass are both significantly increased by 11% in Etomoxir-treated rats[4].

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

    分子量

    326.82

    Formula

    C₁₇H₂₃ClO₄

    CAS 号
    中文名称

    乙莫克舍;依莫克舍

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    -20°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    溶解性数据
    In Vitro: 

    DMSO : 140 mg/mL (428.37 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.0598 mL 15.2989 mL 30.5979 mL
    5 mM 0.6120 mL 3.0598 mL 6.1196 mL
    10 mM 0.3060 mL 1.5299 mL 3.0598 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 (protect from light, stored under nitrogen)。-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    90% (20% SBE-β-CD in saline)

      Solubility: 3.5 mg/mL (10.71 mM); Suspended solution; Need ultrasonic

      此方案可获得 3.5 mg/mL (10.71 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 35.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 2.

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

      Solubility: ≥ 3.5 mg/mL (10.71 mM); Clear solution

      此方案可获得 ≥ 3.5 mg/mL (10.71 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 35.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 3.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (7.65 mM); Clear solution; Need ultrasonic

      此方案可获得 2.5 mg/mL (7.65 mM) 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
    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    Cell Assay
    [2]

    Rat heart H9c2 myoblastic cells are incubated in DMEM containing 10% fetal bovine serum until near confluence. In some experiments, cells are preincubated for 2 h with DMEM (serum-free) in the absence or presence of 1-80 μM Etomoxir and then incubated for 2 h with 0.1 mM [1-14C]oleic acid (10 μCi/dish, binds to BSA in a 1:1 molar ratio). In other experiments, cells are preincubated for 2 h plus or minus 40 μM Etomoxir and then incubated for 2 h with 0.1 μM or 0.1 mM [1,3-3H]glycerol (10 μCi/dish), 0.1 mM [1-14C]oleic acid (2 μCi/dish, binds to BSA in a 1:1 molar ratio), 0.1 mM [1-14C]palmitic acid (2 μCi/dish, binds to BSA in a 1:1 molar ratio), 28 μM [methyl-3H]choline (2 μCi/dish), 0.4 mM [3H]serine (20 μCi/dish), or 40 μM myo-[3H]inositol (10 μCi/dish). The medium is removed and the cells washed twice with ice-cold saline and then harvested from the dish with 2 mL methanol-water (1:1, v/v) for lipid extraction. An aliquot of the homogenate is taken for the determination of total uptake of radioactivity into cells. Phospholipids are then isolated and radioactivity in these determined[2].

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

    Animal Administration
    [3][4]

    Mice[3]
    80 male C57BLKS/J lar-Leprdb/db mice and 20 wild type littermates (8 week) are used. db/db mice are randomly divided into four groups: db/db group, Etomoxir group, MitoQ group, and PFT-α group. In the Etomoxir group, mice are intraperitoneally injected with 1 mg/kg Etomoxir twice every week. In the MitoQ group, 50 μM MitoQ is given to the mice in water. Water bottles, containing either MitoQ, are covered with aluminum foil, and all bottles are refilled every 3 days. In the PFT-α group, mice are intraperitoneally injected with 1 mg/kg PFT-α twice every week. WT mice are administrated with vehicle instead. The experimental period is 8 weeks. At the end, peripheral blood samples and bone marrow cells are harvested for the assays.
    Rats[4]
    Male Lewis rats, weighing 150-200 g, are used in the present study. Animals are kept on a 12 h:12 h light/dark cycle and fed a Purina Chow diet and water ad libitum. The rats are divided into two groups: (1) control and (2) Etomoxir. Etomoxir (20 mg/kg of body weight) is dissolved in 0.9% (w/v) NaCl and administered intraperitoneally for 8 days. Control rats receive saline. The last injection is given 24 h before the experiment.

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

    参考文献

    Purity: 99.65%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    Etomoxir
    目录号:
    HY-50202
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