Home Metabolism CPT inhibitor Etomoxir sodium salt

연구용

Etomoxir sodium salt CPT-1 inhibitor

제품 번호: S8244

Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) 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.
Etomoxir sodium salt CPT inhibitor Chemical Structure

화학 구조

분자량: 320.74

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품질 관리 (Quality Control)

배치: 순도: 99.87%
99.87

함께 자주 사용되는 제품 Etomoxir sodium salt

BPTES

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

UK-5099 (PF-1005023)

It 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.

Alisertib (MLN8237)

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

Trimetazidine

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

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
KB cells Cytotoxicity assay Cytotoxicity in human KB cells, IC50=2.76 μM 21504156
U251 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
U373-U Growth inhibiton assay 50 μM 72-h treatments have slight growth inhibitory effects 30574020
MCF-7 cells Function assay 0–200 μM 4 h in db-cAMP-exposed cells ETO caused a metabolic imbalance 30981740
HepG2 cells Function assay 24 h Etomoxir significantly inhibits palmitate metabolism with an IC50 in the nanomolar range. 29740314
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 320.74 화학식

C15H18ClO4.Na

 보관 (수령일로부터)
CAS 번호 828934-41-4 SDF 다운로드 원액 보관

동의어 (R)-(+)-Etomoxir sodium salt Smiles C1C(O1)(CCCCCCOC2=CC=C(C=C2)Cl)C(=O)[O-].[Na+]

용해도 (Solubility)

In vitro
배치:

DMSO : 64 mg/mL (199.53 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
CPT-1
PPARα
시험관 내(In vitro)
Etomoxir sodium salt has also been identified as a direct agonist of PPARα. This compound 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. It reduces pro-inflammatory cyokine production and increases apoptosis of MOG specific T cells. Etomoxir has been shown to decrease oxygen consumption rates (OCRs) and impair ATP and NADPH production in the pediatric glioblastoma cell line SF188.
생체 내(In vivo)
Etomoxir sodium salt 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. This compound 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 this chemical 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, it has a selective influence on the rate of contraction and relaxation of overloaded hearts. This compound, in the liver can act as peroxisomal proliferator, increasing DNA synthesis and liver growth. Etomoxir-treated mice displays a reduced immune cell infiltration in the CNS with few macrophages, activated microglia, or T cells present. It reduces inflammation and demyelination in the CNS of treated mice. Inhibition of fatty acid oxidation by this chemical 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. It 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.
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적용 분야 (Applications)

방법 바이오마커 이미지 PMID
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
S8244-WB1
26716645