(R)-(+)-Etomoxir sodium salt
(Synonyms: (R)-(+)-乙莫克舍钠盐,(R)-(+)-Etomoxir sodium salt) 目录号 : GC15104
(R)-(+)-Etomoxir sodium salt(Etomoxir; ETO)是一种用于代谢和心血管疾病的小分子,经酶转化为活性抑制剂乙托莫西里尔辅酶a (IC50 约为0.01-0.70 µM)后,对CPT-1a和CPT-1b的抑制表现出纳摩尔效价。
Cas No.:828934-41-4
Sample solution is provided at 25 µL, 10mM.
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(R)-(+)-Etomoxir sodium salt(Etomoxir) is a small molecule developed for metabolic and cardiovascular disease that exhibits nanomolar potency toward CPT-1a and CPT-1b upon enzymatic conversion to the active inhibitor etomoxiryl CoA (IC50 = 0.01-0.70 µM) [1-3].
Etomoxir (50 µM ETO; every other day in 10days) reduces CD28-costimulated T cell proliferation without affecting T cell effector differentiation[4]. Low concentrations(3µM,24h) of etomoxir effectively inhibit CPT-1 but do not affect M(IL-4) polarization, High concentrations of Etomoxir (200 µM) inhibit M(IL-4) polarization independently of CPT-1 activity in BMDM cells[5]. Besides the effect of etomoxil on T cell differentiation and function was independent of Cpt1a expression [6].
Etomoxir (40 mg/kg;i.p; every other day for 20 days) suppressed human bladder cancer (BCa) cell growth in vivo[7]. Etomoxir (i.p; 1 mg/kg Etomoxir; twice every week) significantly inhibits the decrease of bone mineral density (BMD) and bone breaking strength in db/db and high fat (HF)-fed mice and suppresses the reduction of BMSCs-differentiated osteoblasts [8].
References:
[1]. O'Connor RS, Guo L, et,al.The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations. Sci Rep. 2018 Apr 19;8(1):6289. doi: 10.1038/s41598-018-24676-6. PMID: 29674640; PMCID: PMC5908836.
[2]. Divakaruni AS, Hsieh WY, et,al. Etomoxir Inhibits Macrophage Polarization by Disrupting CoA Homeostasis. Cell Metab. 2018 Sep 4;28(3):490-503.e7. doi: 10.1016/j.cmet.2018.06.001. Epub 2018 Jun 28. PMID: 30043752; PMCID: PMC6125190.
[3]. Ceccarelli SM, Chomienne O, et,al. Carnitine palmitoyltransferase (CPT) modulators: a medicinal chemistry perspective on 35 years of research. J Med Chem. 2011 May 12;54(9):3109-52. doi: 10.1021/jm100809g. Epub 2011 Apr 19. PMID: 21504156.
[4]. O'Connor RS, Guo L, et,al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations. Sci Rep. 2018 Apr 19;8(1):6289. doi: 10.1038/s41598-018-24676-6. PMID: 29674640; PMCID: PMC5908836.
[5]. Divakaruni AS, Hsieh WY, et,al. Etomoxir Inhibits Macrophage Polarization by Disrupting CoA Homeostasis. Cell Metab. 2018 Sep 4;28(3):490-503.e7. doi: 10.1016/j.cmet.2018.06.001. Epub 2018 Jun 28. PMID: 30043752; PMCID: PMC6125190.
[6]. Raud B, Roy DG, et,al. Etomoxir Actions on Regulatory and Memory T Cells Are Independent of Cpt1a-Mediated Fatty Acid Oxidation. Cell Metab. 2018 Sep 4;28(3):504-515.e7. doi: 10.1016/j.cmet.2018.06.002. Epub 2018 Jun 28. PMID: 30043753; PMCID: PMC6747686.
[7]. Cheng S, Wang G, et,al.Fatty acid oxidation inhibitor etomoxir suppresses tumor progression and induces cell cycle arrest via PPARγ-mediated pathway in bladder cancer. Clin Sci (Lond). 2019 Aug 7;133(15):1745-1758. doi: 10.1042/CS20190587. PMID: 31358595.
[8]. Li J, He W, et,al.FFA-ROS-P53-mediated mitochondrial apoptosis contributes to reduction of osteoblastogenesis and bone mass in type 2 diabetes mellitus. Sci Rep. 2015 Jul 31;5:12724. doi: 10.1038/srep12724. PMID: 26226833; PMCID: PMC4521203.
(R)-(+)-Etomoxir sodium salt(Etomoxir; ETO)是一种用于代谢和心血管疾病的小分子,经酶转化为活性抑制剂乙托莫西里尔辅酶a (IC50 约为0.01-0.70 µM)后,对CPT-1a和CPT-1b的抑制表现出纳摩尔效价[1-3]。
Etomoxir能减少CD28共刺激的T细胞增殖而不影响T细胞效应分化[4]。低浓度(3µM,24h) Etomoxir可有效抑制CPT-1,但不影响M(IL-4)极化,高浓度(200 µM) Etomoxir可抑制BMDM细胞中M(IL-4)极化,而不影响CPT-1活性[5]。Etomoxir对T细胞分化和功能的影响不依赖于Cpt1a的表达[6]。
Etomoxir (40 mg/kg;i.p; every other day for 20 days)体内抑制人膀胱癌(BCa)细胞生长[7]。Etomoxir(i.p; 1 mg/kg Etomoxir; twice every week)抑制db/db和高脂喂养小鼠骨密度(BMD)和骨折强度的下降,抑制BMSCs分化成骨细胞的减少[8]。
| Cell experiment [1]: | |
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Cell lines |
Human T cells |
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Preparation Method |
Activated T cells (day 3) were treated with 50 µM (R)-(+)-Etomoxir sodium salt every other day throughout logarithmic expansion. |
|
Reaction Conditions |
50 µM Etomoxir; every other day in 10days |
|
Applications |
Etomoxir reduces CD28-costimulated T cell proliferation without affecting T cell effector differentiation. |
| Animal experiment [2]: | |
|
Animal models |
Male BALB/c nude mice (3 weeks old) |
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Preparation Method |
Mice with approximately 3 mm tumors(T24 cells)were assigned to two groups (n=5) randomly. Etomoxir (40 mg/kg) and vehicle were injected intraperitoneally every other day for 20 days. |
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Dosage form |
40 mg/kg;i.p; every other day for 20 days |
|
Applications |
Etomoxir suppressed human bladder cancer (BCa) cell growth in vivo. |
|
References: [1]. O'Connor RS, Guo L, et,al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations. Sci Rep. 2018 Apr 19;8(1):6289. doi: 10.1038/s41598-018-24676-6. PMID: 29674640; PMCID: PMC5908836. |
|
| Cas No. | 828934-41-4 | SDF | |
| 别名 | (R)-(+)-乙莫克舍钠盐,(R)-(+)-Etomoxir sodium salt | ||
| 化学名 | sodium (R)-2-(6-(4-chlorophenoxy)hexyl)oxirane-2-carboxylate | ||
| Canonical SMILES | ClC1=CC=C(C=C1)OCCCCCC[C@@]2(C([O-])=O)OC2.[Na+] | ||
| 分子式 | C15H18ClNaO4 | 分子量 | 320.74 |
| 溶解度 | ≥ 50mg/mL in DMSO，≥ 5mg/mL in H2O | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1178 mL | 15.589 mL | 31.1779 mL |
| 5 mM | 0.6236 mL | 3.1178 mL | 6.2356 mL |
| 10 mM | 0.3118 mL | 1.5589 mL | 3.1178 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet