CAS: 519-09-5; Ecgonine Benzoate

上下游产品

benzoic acid anhydride ecgonine C°Caine (-)-c°Caine hydr°ChlorideC°Caine c°Caethylene RTI 13 ecgonine

📜古卡因置于human Carboxylesterase 1B,Recombinant体系中,用 Aq. Phosphate Buffer 作为反应溶剂,化学反应 1.0H,反应生成 苯甲醯艾克寧
参考文献:羧酸酯酶依赖性达比加群酯水解的鉴定.
标题:羧酸酯酶依赖性达比加群酯水解的鉴定.
摘要:达比加群酯 (Dabe) 是一种口服前药,可通过丝氨酸酯酶迅速转化为活性凝血酶抑制剂达比加群 (Dab).本研究的目的是研究人羧酸酯酶水解 Dabe 的体外动力学和途径,以及酒精对这些转化的影响.测定了两种人重组羧酸酯酶(ces1 和 Ces2)以及人肠道微粒体和人肝脏 S9 级分中 Dabe 水解的动力学.还检查了酒精(一种已知的 Ces1 抑制剂)对羧酸酯酶和人肝 S9 级分中 Dabe 代谢物形成的影响.研究了双(4-硝基苯基)磷酸酯对羧酸酯酶介导的 Dabe 代谢的抑制作用以及酒精对经典羧酸酯酶底物(可卡因)水解的影响,以验证体外模型.dabe 的乙酯仅被 Ces1 水解为 M1(km 24.9 +/-2.9 μm,Vmax 676 +/-26 Pmol/min 每毫克蛋白质),而 Dabe 的氨基甲酸酯仅被 Ces2 水解为 M2(km 5.5 +/-0.8 μm; Vmax 71.1
DOI:10.1124/dmd.113.054353

专利信息

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:US-4708929-A
优先权日:1984-10-29
标 题:Methods for protein binding enzyme complementation assays
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 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.