McN3716 (Methyl palmoxirate)
(Synonyms: Methyl palmoxirate; NSC359682) 目录号 : GC31427
McN3716 (Methyl palmoxirate) 是肉碱棕榈酰转移酶 I (CPT-1) 抑制剂。
Cas No.:69207-52-9
Sample solution is provided at 25 µL, 10mM.
McN3716 is a carnitine palmitoyltransferase I (CPT-1) inhibitor.
Inhibition of brain mitochondrial β-oxidation by McN3716 (Methyl palmoxirate, MEP) significantly reduces the levels of all measured HETE and epoxytrienoic acids (EET), nonenzymatic auto-oxidative metabolites of ARA, by 23% to 44% and 32% to 50% compared with vehicle-injected rats, respectively, except for 15-HETE which was unaffected. There is a significant 34% reduction in the level of 6-keto-PGF1α, a byproduct of PGI2 (prostacyclin) in McN3716-treated rats. Similarly, the brain level of hydroxyeicosapentaenoic acids, nonenzymatic auto-oxidative metabolites of EPA, is reduced by 35% to 76% upon McN3716 treatment relative to vehicle[1].
[1]. Chen CT, et al. Inhibiting mitochondrial β-oxidation selectively reduces levels of nonenzymatic oxidative polyunsaturated fatty acid metabolites in the brain. J Cereb Blood Flow Metab. 2014 Mar;34(3):376-9.
Animal experiment: | Rats[1] Male Sprague Dawley rats are used. The rats receive ad libitum access to standard chow and water. At 15 weeks of age, six rats were subjected to either high-energy, head-focused microwave irradiation or CO2 asphyxiation. A separate group of 11 rats were implanted with a tail vein catheter (intravenous catheter 24 gauge/0.75 inch) and received either an intravenous injection of vehicle or 10 mg/kg of McN3716. Fifteen minutes after injection, rats were rapidly euthanized by high-energy, head-focused microwave irradiation (13.5 kW for 1.6 seconds) to avert ischemia for accurate quantification of in vivo basal levels of nonenzymatic auto-oxidative PUFA metabolites and enzymatically derived metabolites. Previously, we reported that this method reduced β-oxidation of fatty acid by 23% to 74%. McN3716 (Methyl palmoxirate, MEP) readily crosses the blood–brain barrier with a plasma half-life of 0.6 minute in the rat. The brain was excised and stored at -80°C for lipidomics profiling. |
References: [1]. Chen CT, et al. Inhibiting mitochondrial β-oxidation selectively reduces levels of nonenzymatic oxidative polyunsaturated fatty acid metabolites in the brain. J Cereb Blood Flow Metab. 2014 Mar;34(3):376-9. |
Cas No. | 69207-52-9 | SDF | |
别名 | Methyl palmoxirate; NSC359682 | ||
Canonical SMILES | O=C(C1(CCCCCCCCCCCCCC)OC1)OC | ||
分子式 | C18H34O3 | 分子量 | 298.46 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 3.3505 mL | 16.7527 mL | 33.5053 mL |
5 mM | 0.6701 mL | 3.3505 mL | 6.7011 mL |
10 mM | 0.3351 mL | 1.6753 mL | 3.3505 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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