Etomoxir sodium salt

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

828934-41-4

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品名称

(R)-(+)-Etomoxir sodium salt

产品介绍

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

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^[1].

IC₅₀& Target

CPT-1a^[2]

体外研究
(In Vitro)

Etomoxir mediates differential metabolic channeling of fatty acid and glycerol precursors into cardiolipin in H9c2 cells^[2].
Etomoxir does not affect the activities of the cardiolipin biosynthetic and remodeling enzymes but causes a reduction in [1-¹⁴C]palmitic acid or [1-¹⁴C]oleic acid incorporation into cardiolipin^[2].
Etomoxir increases [1,3-³H]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^[2].

Cell Viability Assay^[2]

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^[3].
Etomoxir inhibits the increase of mitochondrial ROS generation in db/db and HF-fed mice and osteoblasts^[3].
Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates^[4]

Animal Model:	80 male C57BLKS/J lar-Lepr^db/dbmice^[3]
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^[4]
Dosage:	20 mg/kg
Administration:	Injected daily; for 8 days
Result:	Etomoxir-treated rats displayed a 44% reduced cardiac CPT-I activity.

分子量

320.74

性状

Solid

Formula

C₁₅H₁₈ClNaO₄

CAS 号

828934-41-4

中文名称

乙莫克舍钠盐；(R)-(+)-乙莫克舍钠盐；(+)-乙莫克舍钠盐

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

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

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.1178 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

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℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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： PBS
Solubility: 3.33 mg/mL (10.38 mM); Clear solution; Need ultrasonic
2.
请依序添加每种溶剂： 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 ddH2O 中，得到澄清透明的生理盐水溶液
3.
请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 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.
请依序添加每种溶剂： 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。

*以上所有助溶剂都可在本网站选购。