CAS: 575-03-1; 7-Hydroxy-4-(Trifluoromethyl)Coumarin

该化合物是科马林家族的合成有机化合物,其特征为丙烯菊酯脊椎骨,其特点是以芳香特性和生物活动著称的苯丙烯酮结构结构;7-位置的氢氧基和4位置的三氟甲基组的存在,对其化学行为和再活动有重大影响;该化合物通常是黄色的黄固态,在乙醇和二甲基硫氧化物等有机溶剂中溶解,但水溶性有限;7-Hydroxy-4-(三氟-甲基)丙烯烃的显露水氟芳烃,在各种应用中有用,包括作为生物化学实验中的荧光探针探针和光动力学疗法的潜在剂;该化合物独特的结构特征有助于其作为生物活性分子的潜力,研究显示各种药性特性,包括抗微生物和抗癌活动.然而,但处理环境应顾及某些毒性.

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CAS号372-31-6 三氟乙酰乙酸乙酯 | CAS号108-46-3 间苯二酚 | CAS号70961-05-6 3-三氟乙酰基丙酸乙酯 | CAS号220001-53-6 7-苄氧基-4-三氟甲基香豆素 | CAS号575-04-2 7-甲氧基-4-(三氟甲基)香豆素 | CAS号1407499-96-0 2,4-dibromo-6-(... | CAS号220001-53-6 7-苄氧基-4-三氟甲基香豆素 | CAS号195210-09-4 4-Trifluorometh... | CAS号575-04-2 7-甲氧基-4-(三氟甲基)香豆素

合成工艺路线路线简述

    7-苄氧基-4-三氟甲基香豆素置于feline Cytochrome P450 1A2 Isoform体系中,用 Aq. Phosphate Buffer 作为反应溶剂,化学反应 0.08H,反应生成 7-羟基-4-三氟甲基香豆素
    参考文献:使用荧光底物对四种猫科动物p450细胞色素的功能性表达和比较表征.
    标题:使用荧光底物对四种猫科动物p450细胞色素的功能性表达和比较表征.
    摘要:1.细胞色素p450(cyp)是人类和其他哺乳动物中异生素的主要代谢酶.cyp同工型在家猫(一种专食的食肉动物)中的特性目前尚不清楚.在这项研究中,我们研究了9种重要的猫cyp亚型在组织中的相对表达和酶学性质. 2. Cyp2E2转录本在猫肝中含量最高,其次是cyp2A13和2E1.肝脏中也存在cyp3A131,1A2和1A1的转录本,而cyp2D6和3A132仅略有表达.cyp3A131是小肠的主要转录本. 3.猫肝和小肠中的四种主要cyp亚型(cyp1A2,Cyp2A13,Cyp2E2和cyp3A131)在大肠杆菌中异源表达,以反应生成功能性单加氧酶系统.我们进行了对17种已知在其他哺乳动物中是cyp亚型抑制剂的测试化合物的筛选,以及两种抗癌药物,以评估使用荧光底物的猫cyp亚型的活性调节.这些cyp亚型对其他抑制剂的选择性总体上与其他哺乳动物中的cyp同工型相似,但有许多例外. 4.本研
    DOI:10.1080/00498254.2016.1257172

    海关参考信息

    专利信息


    专利号:US-5362625-A
    优先权日:1991-05-15
    标 题:Methods and compositions for enzyme complementation assays using the omega region of β-galactosidase
    发明人:KREVOLIN MARK; KATES DAVID
    权利人:MICROGENICS CORP
    摘要:The use of omega-acceptor and omega-donor polypeptides (comprising about two-thirds and one-third of the beta -galactosidase molecule amino and carboxyl termini, respectively), prepared by recombinant DNA techniques, DNA synthesis, or chemical polypeptide synthesis techniques, which are capable of interacting to form an active enzyme complex having catalytic activity characteristic of beta -galactosidase, is described along with improved methods and novel compositions for enzyme complementation assays for qualitative and quantitative determination of a suspected analyte in a sample.

    专利号:US-7223541-B2
    优先权日:2001-08-29
    标 题:Terminal-phosphate-labeled nucleotides and methods of use
    发明人:FULLER CARL; KUMAR SHIV; SOOD ANUP; NELSON JOHN
    权利人:GE HEALTHCARE BIO SCIENCES
    摘要:The present invention relates to improved methods of detecting a target using a labeled substrate or substrate analog. The methods comprise reacting the substrate or substrate analog in an enzyme-catalyzed reaction which produces a labeled moiety with independently detectable signal only when such substrate or substrate analog reacts. The present invention, in particular, describes methods of detecting a nucleic acid in a sample, based on the use of terminal-phosphate-labeled nucleotides as substrates for nucleic acid polymerases. The methods provided by this invention utilize a nucleoside polyphosphate, dideoxynucleoside polyphosphate, or deoxynucleoside polyphosphate analogue which has a colorimetric dye, chemiluminescent, or fluorescent moiety, a mass tag or an electrochemical tag attached to the terminal-phosphate. When a nucleic acid polymerase uses this analogue as a substrate, an enzyme-activatable label would be present on the inorganic polyphosphate by-product of phosphoryl transfer. Cleavage of the polyphosphate product of phosphoryl transfer via phosphatase leads to a detectable change in the label attached thereon. When the polymerase assay is performed in the presence of a phosphatase, there is provided a convenient method for real-time monitoring of DNA or RNA synthesis and detection of a target nucleic acid.

    专利号:US-7052839-B2
    优先权日:2001-08-29
    标题 :Terminal-phosphate-labeled nucleotides and methods of use
    发明人:NELSON JOHN; FULLER CARL; SOOD ANUP; KUMAR SHIV
    权利人:AMERSHAM BIOSCIENCES CORP
    摘要:The present invention describes methods of detecting a nucleic acid in a sample, based on the use of terminal-phosphate-labeled nucleotides as substrates for nucleic acid polymerases. The methods provided by this invention utilize a nucleoside polyphosphate, dideoxynucleoside polyphosphate, or deoxynucleoside polyphosphate analogue which has a colorimetric dye, chemiluminescent, or fluorescent moiety, a mass tag or an electrochemical tag attached to the terminal-phosphate. When a nucleic acid polymerase uses this analogue as a substrate, an enzyme-activatable label would be present on the inorganic polyphosphate by-product of phosphoryl transfer. Cleavage of the polyphosphate product of phosphoryl transfer via phosphatase leads to a detectable change in the label attached thereon. When the polymerase assay is performed in the presence of a phosphatase, there is provided a convenient method for real-time monitoring of DNA or RNA synthesis and detection of a target nucleic acid.

    专利号:US-5643734-A
    优先权日:1984-03-01
    标题 :Methods for protein binding enzyme complementation assays
    发明人:HENDERSON DANIEL ROBERT
    权利人:MICROGENICS CORP
    摘要:This invention relates to improved methods and novel compositions for enzyme complementation assays for qualitative and quantitative determination of a suspected analyte in a sample. The use of enzyme-acceptor and enzyme-donor polypeptides prepared by recombinant DNA techniques, DNA synthesis or chemical polypeptide synthesis techniques which are capable of interacting to form an active enzyme complex having catalytic activity characteristic of beta -galactosidase is described. Both homogeneous and heterogeneous assays utilizing these polypeptides are described.

    专利号:US-5120653-A
    优先权日:1985-04-08
    标 题:Vector comprising DNA sequence coding for enzyme-donor polypeptide
    发明人:HENDERSON DANIEL R
    权利人:MICROGENICS CORP
    摘要:This invention relates to improved methods and novel compositions for enzyme complementation assays for qualitative and quantitative determination of a suspected analyte in a sample. The use of enzyme-acceptor and enzyme-donor polypeptides prepared by recombinant DNA techniques, DNA synthesis or chemical polypeptide synthesis techniques which are capable of interacting to form an active enzyme complex having catalytic activity characteristic of beta -galactosidase is described. Both homogeneous and heterogeneous assays utilizing these polypeptides are described.

    专利号:EP-0199801-B1
    优先权日:1984-10-29
    标 题:Methods for protein binding enzyme complementation assays
    摘要:Improved methods and novel compositions for enzyme complementation assays for qualitative and quantitative determination of a suspected analyte in a sample. The use of enzyme-acceptor and enzyme-donor polypeptides prepared by recombinant DNA techniques, DNA synthesis or chemical polypeptide synthesis techniques which are capable of interacting to form an active enzyme complex having catalytic activity characteristics of beta-galactosidase is described. Both homogeneous and heterogeneous assays utilizing these polypeptides are described.
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    主要参考文献

    [参考文献]: Renwick Ab, Et, Al. Evaluation Of 7-Benzyloxy-4-Trifluoromethylcoumarin, Some Other 7-Hydroxy-4-Trifluoromethylcoumarin Derivatives And 7-Benzyloxyquinoline As Fluorescent Substrates For Rat Hepatic Cytochrome P450 Enzymes. Xenobiotica. 2001 Dec;31(12):861-78.
    [参考文献]: Changning Wang, Et Al. Design, Synthesis, And Evaluation Of Coumarin-Based Molecular Probes For Imaging Of Myelination. J Med Chem. 2011 Apr 14;54(7):2331-40.
    [参考文献]: H T Huynh, Et Al. Effects Of Plant-Derived Phenols On Rat Liver Cytochrome P450 2B1 Activity. Anticancer Res. 2002 May-Jun;22(3):1699-703.
    [参考文献]: Iva Bouová, Et Al. Influence Of Diet Supplementation With Green Tea Extract On Drug-Metabolizing Enzymes In A Mouse Model Of Monosodium Glutamate-Induced Obesity. Eur J Nutr. 2016 Feb;55(1):361-71.
    [参考文献]: James R Reed, Et Al. Environmentally Persistent Free Radical-Containing Particulate Matter Competitively Inhibits Metabolism By Cytochrome P450 1A2. Toxicol Appl Pharmacol. 2015 Dec 1;289(2):223-30.

    合成参考文献


    摘要:Cheng, B.; Wang, T., Science of Synthesis Knowledge Updates, (2020) 3, 183.
    摘要:Cheng, B.; Wang, T., Science of Synthesis Knowledge Updates, (2020) 3, 186.
    摘要:Cheng, B.; Wang, T., Science of Synthesis Knowledge Updates, (2020) 3, 177.
    摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198
    参考文献:10.1007/s00228-002-0426-9
    摘要:Thapar MM, Ashton M, Lindegårdh N, Bergqvist Y, Nivelius S, Johansson I, Björkman A. Time-dependent pharmacokinetics and drug metabolism of atovaquone plus proguanil (Malarone) when taken as chemoprophylaxis. European Journal of Clinical Pharmacology. 2002 Feb 28;58(1):19–27. doi: 10.1007/s00228-002-0426-9.
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