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化合物简介
Efaproxiral (INN) is an analogue of the cholesterol drug bezafibrate developed for the treatment of depression, traumatic brain injury, ischemia, stroke, myocardial infarction, diabetes, hypoxia, sickle cell disease, hypercholesterolemia and as a radio sensitiser. The chemical is a propanoic acid in the class of amphipathic carboxylic acids. Most propanoic acid produced is consumed as a preservative for both animal feed and food for human consumption. One use for efaproxiral is to increase the efficacy of certain chemotherapy drugs which have reduced efficacy against hypoxic tumours, and can thus be made more effective by increased offloading of oxygen into the tumour tissues. No benefit was seen for efaproxiral in phase III clinical trials. The increased oxygenation of tissues could theoretically also produce enhanced exercise capacity in feline, rat and canine models for approximately 100 min. immediately after a high dosage 45 min. intravenous infusion. This has led World Anti-Doping Agency to categorise efaproxiral under a prohibited method to artificially enhance the uptake, transport or delivery of oxygen. There is no existing evidence that efaproxiral can effectively enhance performance in humans. Efaproxiral can be absorbed via transdermal, rectal, inhalation and gastrointestinal routes, though not at plasma concentrations great enough to alter the oxygen-haemoglobin dissociation curve. Efaproxiral is explicitly excluded from the 2012 World Anti-Doping Agency list of Prohibited Substances and is explicitly included in the Prohibited Methods section M1 as a forbidden procedure to alter the oxygen-haemoglobin dissociation curve in order to allosterically modify haemoglobin.
基本信息
CAS:131179-95-8
中文别名:2-(4-(((3,5-二甲基苯胺)羰基)甲基)苯氧基)-2-甲基丙酸;
英文别名:2-Dacmpp;Efaproxyn;2-[4-((((3,5-dimethylphenyl)-amino)carbonyl)methyl)phenoxy]-2-methyl propionic acid;RSR13;2-(4-(((3,5-dimethylanilino)carbonyl)methyl)phenoxy)-2-methylpropionic acid;Efaproxiral;2-(4-(2-((3,5-Dimethylphenyl)amino)-2-oxoethyl)phenoxy)-2-methylpropanoic acid;
分子式:C20H23NO4
分子量:341.401
精确质量:341.163
Psa:75.63
Logp:3.7996
中文别名:2-(4-(((3,5-二甲基苯胺)羰基)甲基)苯氧基)-2-甲基丙酸;
英文别名:2-Dacmpp;Efaproxyn;2-[4-((((3,5-dimethylphenyl)-amino)carbonyl)methyl)phenoxy]-2-methyl propionic acid;RSR13;2-(4-(((3,5-dimethylanilino)carbonyl)methyl)phenoxy)-2-methylpropionic acid;Efaproxiral;2-(4-(2-((3,5-Dimethylphenyl)amino)-2-oxoethyl)phenoxy)-2-methylpropanoic acid;
分子式:C20H23NO4
分子量:341.401
精确质量:341.163
Psa:75.63
Logp:3.7996
编号系统
物化性质
密度:1.202g/cm3
沸点:554.5ºC at 760mmHg
闪点:289.2ºC
折射率:1.597
蒸汽压:3.93E-13mmHg at 25°C
沸点:554.5ºC at 760mmHg
闪点:289.2ºC
折射率:1.597
蒸汽压:3.93E-13mmHg at 25°C
安全信息
海关编码:2924299090
生产方法及用途
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上游原料
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图谱
13C NMR : Predict

1H NMR : Predict
