(R)-(+)-Etomoxir sodium salt (Synonyms: (R)(+)Etomoxir) |
| カタログ番号GC15104 |
(R)-(+)-Etomoxir sodium saltは代謝の疾患と心血管疾患のために開発された低分子であり、酵素を介して活性阻害剤であるetomoxiryl CoA(IC50 = 0.01-0.70 µM)に変換された後、CPT-1aとCPT-1bに対してナノモルの効力を示す。
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.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
(R)-(+)-Etomoxir sodium saltは代謝の疾患と心血管疾患のために開発された低分子であり、酵素を介して活性阻害剤であるetomoxiryl CoA(IC50 = 0.01-0.70 µM)に変換された後、CPT-1aとCPT-1bに対してナノモルの効力を示す。
Etomoxir（50µM ETO；1日おきに10日間）はCD28と一緒に刺激するT細胞の増殖を減少することができるだけでなく、T細胞エフェクター分化に影響を与えない。低濃度（3µM，24時間）のEtomoxirはCPT-1の効果を阻害することができるが、M（IL-4）の分極化に影響を与えない。高濃度（200µM）のEtomoxirはBMDM細胞のM（IL-4）の分極を阻害することができるが、CPT-1の活性と無関係である。また、T細胞の分化と機能に対するEtomoxirの効果はCpt1aの発現には依存したかった。
Etomoxir（40 mg/kg；腹腔内に注射；1日おきに20日間）は体にヒトの膀胱がん（BCa）細胞の増殖を阻害した。Etomoxir（i.p；Etomoxir 1mg/kg；毎週2回）db/dbと高脂肪（HF）で養うマウスにおける骨密度（BMD）と骨折の強度の低下を顕著に抑制し、BMSCsによる骨細胞への分化の減少を抑制した。
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.
| 細胞実験[1]: | |
細胞株 | ヒト T 細胞 |
準備方法 | 活性化されたT細胞（第3日）は対数の展開の期間以内に1日おきに50µMの(R)-(+)-Etomoxir sodium saltを処理する。 |
反応条件 | 50 µMのEtomoxir; 1日おきに10日間 |
アプリケーション | EtomoxirはCD28と一緒に刺激するT細胞の増殖を減少することができるだけでなく、T細胞エフェクター分化に影響を与えない。 |
| 動物実験 [2]: | |
動物モデル | 雄BALB/c ヌードマウス (3週齢) |
準備方法 | 約3mmの腫瘍（T24细胞）があるマウスをランダムに２つのグループ（n=5）に分ける。Etomoxir（40 mg/kg）と賦形剤を1日おきに腹腔内に投与し、20日間持続する。 |
投与形態 | 40 mg/kg;i.p; 1日おきに20日間 |
アプリケーション | Etomoxirは体にヒトの膀胱がん（BCa）細胞の増殖を阻害した。 |
References: | |
| Cas No. | 828934-41-4 | SDF | |
| 同義語 | (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 |
| 溶解度 | ≥ 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. |
||
| 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *