(R)-(+)-Etomoxir sodium salt|828934-41-4|((R)-(+)-Etomoxir sodium salt)-陌孚医药/Medlife

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(R)-(+)-Etomoxir sodium salt (Synonyms: (R)-(+)-Etomoxir sodium salt)

目录号: PC10197 纯度: ≥98%

CAS No. :828934-41-4

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中文名称	(R)-(+)-Etomoxir sodium salt
中文别名	(2R)-2-[6-(4-氯苯氧基)己基]环氧乙烷甲酸钠;(R)-(+)-乙莫克舍钠盐;钠 (r)-2-(6-(4-氯苯氧基)己基)环氧乙烷-2-羧酸;SODIUM (R)-2-(6-(4-CHLOROPHENOXY)HEXYL)OXIRANE-2-CARBOXYLATE;(R)-2-(6-(4-氯苯氧基)己基)环氧乙烷-2-羧酸钠盐
英文名称	(R)-(+)-Etomoxir sodium salt
英文别名	2-Oxiranecarboxylicacid, 2-[6-(4-chlorophenoxy)hexyl]-, sodium salt (1:1), (2R)-;(+)-Etomoxir (sodium salt);(+)-Etomoxir sodium salt;(R)-(+)-Etomoxir sodium salt;(R)-2-(6-(4-chlorophenoxy)hexyl)oxirane-2-carboxylate sodium salt or (R)-Etomoxir sodium salt;ANTI-EAPII (TTRAP);SODIUM (R)-2-(6-(4-CHLOROPHENOXY)HEXYL)OXIRANE-2-CARBOXYLATE;sodium (S)-2-(6-(4-chlorophenoxy)hexyl)oxirane-2-carboxylate;sodium,(2R)-2-[6-(4-chlorophenoxy)hexyl]oxirane-2-carboxylate
Cas No.	828934-41-4
分子式	C₁₅H₁₈O₄Cl-^.Na+
分子量	320.74
包装储存	-20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

生物活性

Etomoxir((R)-(+)-Etomoxir) sodium salt 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.

性状

Solid

IC50 & Target[1][2]

CPT-1a

体外研究(In Vitro)

Etomoxir mediates differential metabolic channeling of fatty acid and glycerol precursors into cardiolipin in H9c2 cells.
Etomoxir does not affect the activities of the cardiolipin biosynthetic and remodeling enzymes but causes a reduction in [1-C]palmitic acid or [1-C]oleic acid incorporation into cardiolipin.
Etomoxir increases [1,3-H]glycerol incorporation into cardiolipin. The mechanism is a 33% increase in glycerol kinase activity, which produces an increased glycerol flux through the de novo pathway of cardiolipin biosynthesis.

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

Cell Viability Assay

Cell Line:	Rat heart H9c2 myoblastic cells
Concentration:	1-80 μM
Incubation Time:	2 hours
Result:	Reduced the incorporation of [1-14C]fatty acids into CL and PtdGro in H9c2 cardiac myoblast cells but did not affect total incorporation of radioactivity into these cells.

体内研究(In Vivo)

Etomoxir 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.
Etomoxir inhibits the increase of mitochondrial ROS generation in db/db and HF-fed mice and osteoblasts.
Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates

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

Animal Model:	80 male C57BLKS/J lar-Lepr mice
Dosage:	1?mg/kg
Administration:	Intraperitoneally injected; twice every week
Result:	Serum alkaline phosphatase was increased in db/db mice, which event was significantly suppressed by Etomoxir. Serum level of osteocalcin, a marker of bone formation, was reduced in db/db mice and Etomoxir markedly inhibited the reduction of osteocalcin. Serum tartrate-resistant acid phosphatase was elevated in db/db mice which phenomenon was significantly suppressed by Etomoxir.

Animal Model:	Rats
Dosage:	20 mg/kg
Administration:	Injected daily; for 8 days
Result:	Etomoxir-treated rats displayed a 44% reduced cardiac CPT-I activity.

运输条件

Room temperature or refrigerated transportation.

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)

参考文献

[1]. Roddy S OConnor, et al. The CPT1a inhibitor, etomoxir induces severe oxidative stress at commonly used concentrations.Sci Rep. 2018 Apr 19;8(1):6289. [Information]

[2]. Fred Y Xu,et al.Etomoxir mediates differential metabolic channeling of fatty acid and glycerol precursors into cardiolipin in H9c2 cells.J Lipid Res. 2003 Feb;44(2):415-23. [Information]

[3]. Jun Li, 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. [Information]

[4]. Joost J F P Luiken, et al. Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates.Biochem J. 2009 Apr 15;419(2):447-55. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (155.89 mM; Need ultrasonic)

H₂O : 5 mg/mL (15.59 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1178 mL	15.5890 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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 3.33 mg/mL (10.38 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (7.79 mM); Clear solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.79 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 ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.79 mM，饱和度未知) 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 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
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.79 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.79 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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