Etomoxir sodium salt

別名：(R)-(+)-Etomoxir sodium salt

製品コード：S8244 純度：99.87%

Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Etomoxir enhances palmitate-induced cell apoptosis.

CAS No. 828934-41-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 59500	国内在庫あり
100mg	JPY 145500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（42）

製品安全説明書

現在のバッチを見る：純度： 99.87%

99.87

Etomoxir sodium saltと併用されることが多い化合物

BPTES

Etomoxir inhibits CPT1 and BPTES blocks glutaminase GLS1 in tumor-bearing mice.

Corbet C, et al. Cell Metab. 2016 Aug 9;24(2):311-23.

UK 5099

Etomoxir and UK5099 synergistically inhibit mitochondrial fusion dynamics when pre-incubated for 1 h prior to the beginning of the fusion experiment in differentiated PC12 cells.

O'Hara D, et al. Front Mol Neurosci. 2019 Sep 18;12:219.

Trametinib (GSK1120212)

Etomoxir and Trametinib use induces tumor regression and prolongs overall survival of the mice.

Marocchi F, et al. J Invest Dermatol. 2023 Mar 31;S0022-202X(23)01952-8.

Alisertib (MLN8237)

Etomoxir and Alisertib combination use induces tumor regression and prolongs overall survival of the mice.

Marocchi F, et al. J Invest Dermatol. 2023 Mar 31;S0022-202X(23)01952-8.

Trimetazidine

Etomoxir reduces the toxic effect of trimetazidine in quiescence-induced cancer cells.

Ortmayr K, et al. Mol Syst Biol. 2022 Sep;18(9):e10716.

Etomoxir sodium salt関連製品

関連ターゲット	CPT1	もっと見る
関連製品	Perhexiline maleate	もっと見る
関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

CPT阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
MCF-7 cells	Function assay	0–200 μM	4 h	in db-cAMP-exposed cells ETO caused a metabolic imbalance	30981740
U373-U	Growth inhibiton assay	50 μM		72-h treatments have slight growth inhibitory effects	30574020
U87	Growth inhibiton assay	50 μM		72-h treatments have slight growth inhibitory effects	30574020
U251	Growth inhibiton assay	50 μM		72-h treatments have slight growth inhibitory effects	30574020
HepG2 cells	Function assay		24 h	Etomoxir significantly inhibits palmitate metabolism with an IC50 in the nanomolar range.	29740314
KB cells	Cytotoxicity assay			Cytotoxicity in human KB cells, IC50=2.76 μM	21504156
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生物活性

製品説明

Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Etomoxir enhances palmitate-induced cell apoptosis.

Targets

CPT-1 ^[1]

PPARα ^[1]

In Vitro
In vitro	Etomoxir has also been identified as a direct agonist of PPARα. Etomoxir is a compound that binds irreversibly to the catalytic site of CPT-1 inhibiting its activity, but also upregulates fatty acid oxidation enzymes. Transcriptional effects of etomoxir could be due to 1. shift in energy metabolism with increased glucose utilization and 2. PPARalpha activation^[1]. Etomoxir reduces pro-inflammatory cyokine production and increases apoptosis of MOG specific T cells^[2]. Etomoxir has been shown to decrease oxygen consumption rates (OCRs) and impair ATP and NADPH production in the pediatric glioblastoma cell line SF188^[3].
細胞実験	細胞株	Splenocytes
	濃度	100 μM
	反応時間	72 h
	実験の流れ	C57BL/6 mice are immunized with 200 μg MOG_35-55 peptide s.c., and 14 days later splenocytes are isolated and cultured at a concentration of 6×10_⁶ cells/ml in DMEM containing high (4.5 g/L) or low (1 g/L) glucose, 10% FBS 50 μg/ml MOG peptide, and 25 ng/ml IL-12 (R&D systems, Minneapolis, MN) in the presence of vehicle or 100 μM etomoxir. 72 hours later cells are harvested for APO-BrdU staining and supernatants collected for IL-4, IL-17 and IFN-γ ELISA. (MOG:myelin oligodendrocyte glycoprotein)
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	p-ERK / p-p38 / p-JNK / p-FoxO4 p21 / FoxO1 / FoxO3a p-mTOR(S2448) / mTOR / p-S6K(T389) / p-4EBP1 / p-BAD(S112) / cleaved PARP p-ACC2 / p-AMPK / AMPK		26716645

In Vivo
In Vivo	Etomoxir has a protective action on the ischemia/reperfusion injury of the kidney similarly to an established PPARalpha agonist. It has been developed for treating non-insulindependent diabetes mellitus. Etomoxir increases the functional recovery of fatty acid perfused ischemic rat hearts which is unrelated to changes in levels of long-chain acylcarnitines and is attributed to an increased glucose use. A chronic treatment of rats with etomoxir increases the SR Ca2+-ATPase activity, the Ca2+ uptake rate, the number of active Ca2+ pumps E~P, the SERCA2 protein and the SERCA2 mRNA abundance of the heart. At a low dosage, etomoxir has a selective influence on the rate of contraction and relaxation of overloaded hearts. Etomoxir, in the liver can act as peroxisomal proliferator, increasing DNA synthesis and liver growth^[1]. Etomoxir-treated mice displays a reduced immune cell infiltration in the CNS with few macrophages, activated microglia, or T cells present. Etomoxir reduces inflammation and demyelination in the CNS of treated mice^[2]. Inhibition of fatty acid oxidation by etomoxir prolongs survival time in a syngeneic mouse model of malignant glioma and slow tumor growth. Emergence and progression of glioma are delayed upon treatment with the investigational drug etomoxir. Etomoxir has already been tested in phase I/II clinical trials for treating moderate congestive heart failure; this trial is discontinued because 4 patients (of 226 taking the drug) developed unacceptably high liver transaminase levels upon treatment, and the risk of such drastic side effects is deemed sufficient to negate the potential benefit of this drug for these patients^[3].
動物実験	動物モデル	C57BL6/J mice
	投与量	15 mg/kg
	投与経路	i.p.

参考
[1] Rupp H, et al. Herz. 2002, 27(7):621-36. [2] Shriver LP, et al. Sci Rep. 2011, 1:79. [3] Lin H, et al. Neuro Oncol. 2017, 19(1):43-54.

参考

化学情報

分子量	320.74	化学式	C₁₅H₁₈ClO₄.Na
CAS No.	828934-41-4	SDF	Download Etomoxir sodium salt SDFをダウンロードする
Smiles	C1C(O1)(CCCCCCOC2=CC=C(C=C2)Cl)C(=O)[O-].[Na+]
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 64 mg/mL ( (199.53 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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* 必須

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C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):