(R)-(+)-Etomoxir sodium salt (Synonyms: (R)(+)Etomoxir) |
| Catalog No.GC15104 |
(R)-(+)-Etomoxir sodium salt (Etomoxir)은 신진대사 및심혈 관 질환을 위한 소분자로 활성 억제제 etoxomiryl CoA로 효소 변환 후 CPT-1a와 CPT-1b에 대한 변환 활성 효소 억제를 나타낸다(IC50 = 0.01-0.70 µM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 828934-41-4
Sample solution is provided at 25 µL, 10mM.
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(R)-(+)-Etomoxir sodium salt (Etomoxir)은 신진대사 및심혈 관 질환을 위한 소분자로 활성 억제제 etoxomiryl CoA로 효소 변환 후 CPT-1a와 CPT-1b에 대한 변환 활성 효소 억제를 나타낸다(IC50 = 0.01-0.70 µM).
Etomoxir (50 µM ETO; 10일마다 홀수일에 주사)는 CD28 공감각인 T세포의 증식을 줄이는 데에 효과적이지만 T세포의 효과분화에는 영향을 미치지 않는다[4]. 낮은 농도(3µM, 24시간)의 Etomoxir는 CPT-1을 효과적으로 억제하지만 M(IL-4)의 양극화에 영향을 미치지 않는다. 고농도의 Etomoxir (200 µM)는 BMDM 세포에서 CPT-1 활동과는 독립적으로 M(IL-4)의 양극화를 억제한다[5]. 이외에도Etomoxir가 T세포의 분화 및 기능에 대한 영향은 Cpt1a 표현과 무관한다[6].
Etomoxir (40 mg/kg; 복강 주사; 20일간 홀수일에 주사)는 인체 방광암 세포의 성장을 체내에서 억제한다[7]. Etomoxir (복강 주사; 1 mg/kg Etomoxir; 매주 두 번)는 db/db 및 고지방(HF) 골밀도(BMD)와 뼈 부서지기 강도의 감소를 현저하게 억제하고 BMSCs-분화된 성골세포의 감소를 억제한다[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.
| 세포 실험 [1]: | |
세포 라인 | 인간 T 세포 |
제조 방법 | 활성화된 T 세포(3일차)는 로그 성장기 전반에 걸쳐 50 µM (R)-(+)- Etomoxir sodium salt으로 홀수일에 처리되었습니다. |
반응 조건 | 50 µM Etomoxir; 이틀에 한 번, 10일 동안 |
응용 분야 | Etomoxir는 CD28 공감각인 T 세포 증식을 줄이는 데에 효과적이지만 T 세포의 효과 분화에는 영향을 미치지 않는다. |
| 동물 실험 [2]: | |
동물 모형 | 수컷 BALB/c 누드 쥐 (3 주령) |
제조 방법 | 약 3mm 크기의 종양(T24 세포)을 가진 쥐는 두 그룹(n=5)에 무작위로 배정되었습니다. Etomoxir (40 mg/kg)와 차량은 20일 동안 격일로 복강 주사로 주어졌습니다. |
제형 | 40 mg/kg;i.p; 이틀에 한 번, 20일 동안 |
응용 분야 | Etomoxir는 체내에서 인간 방광암(BCa) 세포의 성장을 억제합니다. |
참고문헌: [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]. 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. | |
| Cas No. | 828934-41-4 | SDF | |
| Synonyms | (R)(+)Etomoxir | ||
| Chemical Name | 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+] | ||
| Formula | C15H18ClNaO4 | M.Wt | 320.74 |
| Solubility | ≥ 50mg/mL in DMSO，≥ 5mg/mL in H2O | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Quality Control & SDS
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- Purity: >99.00%
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