Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Etomoxir 是肉碱棕榈酰转移酶 1a (CPT-1a) 抑制剂,通过抑制 CPT-1a 来抑制脂肪酸氧化,且抑制人、大鼠和豚鼠中棕榈酸酯的氧化。Etomoxir 对腺嘌呤核苷酸转位酶有抑制作用,可通过破坏CoA稳态来抑制巨噬细胞极化。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 281 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,420 | 现货 | ||
50 mg | ¥ 3,590 | 现货 | ||
100 mg | ¥ 5,190 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
产品描述 | Etomoxir is a carnitine palmitoyltransferase 1a (CPT-1a) inhibitor that inhibits fatty acid oxidation by inhibiting CPT-1a and inhibits palmitate oxidation in humans, rats, and guinea pigs. Etomoxir has an inhibitory effect on adenine nucleotide translocase and can inhibit macrophage polarization by disrupting CoA homeostasis. |
体外活性 | Etomoxir irreversibly binds to the catalytic site of CPT-1, inhibiting its activity but also upregulating fatty acid oxidase. Etomoxir was developed as an inhibitor of mitochondrial carnitine palmitoyltransferase-1 (CPT-1), which is located on the outer membrane of the mitochondria. Etomoxir, acts as a peroxisome proliferator in the liver, increasing DNA synthesis and liver growth. Therefore, in addition to being a CPT1 inhibitor, etomoclax can also be considered a PPARalpha agonist[1]. Etomoxir is a member of the ethylene oxide carboxylate carnitine palmitoyltransferase I inhibitor family and has been suggested as an inhibitor against heart failure. Acute Etomoxir treatment irreversibly inhibits carnitine palmitoyltransferase I activity. As a result, fatty acid import into mitochondria and β-oxidation are reduced, whereas cytosolic fatty acid accumulation and glucose oxidation are increased. Prolonged incubation (24 hours) with Etomoxir produces differential effects on the expression of several metabolic enzymes.[1] |
体内活性 |
Rats were injected with Etomoxir, daily for 8 days at a dose of 20 mg/kg body weight. Etomoxir-treated rats showed a 44% reduction in cardiac CPT-I activity. Treatment of Lewis rats with 20 mg/kg Etomoxir for 8 days did not alter blood glucose levels, consistent with similar Etomoxir feeding studies. Likewise, Etomoxir feeding did not affect general growth characteristics such as weight gain, nor did it affect hindlimb muscle mass. However, in Etomoxir-treated rats, both heart mass and liver mass were significantly increased by 11%.[3] Etomoxir is an inhibitor of CPT1, a key enzyme involved in free fatty acid (FFA) oxidation. P53 directly interacts with Bax and Bax is inhibited by Etomoxir, further confirming the direct interaction of P53 and Bax and the involvement of FAO-mediated mitochondrial ROS generation in db/db mice.[2] |
别名 | (R)-(+)-Etomoxir |
分子量 | 326.82 |
分子式 | C17H23ClO4 |
CAS No. | 124083-20-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 32.68 mg/mL (100 mM), Sonication and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.0598 mL | 15.2989 mL | 30.5979 mL | 76.4947 mL |
5 mM | 0.612 mL | 3.0598 mL | 6.1196 mL | 15.2989 mL | |
10 mM | 0.306 mL | 1.5299 mL | 3.0598 mL | 7.6495 mL | |
20 mM | 0.153 mL | 0.7649 mL | 1.5299 mL | 3.8247 mL | |
50 mM | 0.0612 mL | 0.306 mL | 0.612 mL | 1.5299 mL | |
100 mM | 0.0306 mL | 0.153 mL | 0.306 mL | 0.7649 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Etomoxir 124083-20-1 Metabolism oxidation-reduction Antioxidant CPT (R)-(+)-Etomoxir Inhibitor inhibitor inhibit