CAS: 62-99-7; 6Beta-Hydroxytestosterone

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CAS号58-22-0 睾酮 | CAS号63-05-8 雄烯二酮 | CAS号2243-06-3 雄甾-4-烯-3β,6β,17β-三醇

📜睾酮置于glucose-6-Phosphate Dehydrogenase,Cyp3A4,Glucose-6-Phosphate,烟酰胺腺嘌呤双核苷酸磷酸盐,Magnesium Chloride体系中,用 Aq. Phosphate Buffer 作为反应溶剂,化学反应 0.17H,反应生成 6,17-二羟基-6B,17B-雄甾-4-烯-3-酮
参考文献:Deoxyschizandrin 是一种天然存在的木脂素,是人类细胞色素 P450 3A 的特异性探针底物.
标题:Deoxyschizandrin 是一种天然存在的木脂素,是人类细胞色素 P450 3A 的特异性探针底物.
摘要:为了准确预测细胞色素 P450 (P450) 3A 酶在代谢过程中所做的修饰,选择最能代表广泛的底物置换范围并遵循 Michaelis-Menten 动力学特性的底物是非常必要的.在本研究中,五味子果实提取物中最丰富的木脂素脱氧五味子素 (Ds) 的氧化途径用人 (Hlm) 和大鼠 (Rlm) 的肝微粒体进行表征.使用液相色谱-质谱法和核磁共振技术仅鉴定了一种单羟基化代谢物 7(S)-羟基化代谢物(异五味子素,Isz).发现 Cyp3A4 和 Cyp3A5 是参与 Ds 单羟基化的主要同种型.还,动力学研究表明,Ds 羟基化在 Hlm 和 Rlm 中均遵循 Michaelis-Menten 动力学.然而,当 Ds 存在时,Isz 的后续代谢几乎不存在.更重要的是,研究了 Ds 与三种充分表征的 Cyp3A 探针底物睾酮 (Tst),咪达唑仑 (Mdz) 和硝苯地平 (Nif) 之间的相互作用.tst
DOI:10.1124/dmd.113.053884

专利信息

专利号:WO-02061120-A1
优先权日:2001-02-01
标题:Method of evaluating ability of drug to induce enzyme in liver cells
发明人：OHTA KUNIHIRO; NAKAGAWA TOSHITO
权利人:CHUGAI PHARMACEUTICAL CO LTD; OHTA KUNIHIRO; NAKAGAWA TOSHITO
摘要:A method of evaluating the ability of a test drug to induce the synthesis of CYP (cytochrome P450) in liver cells characterized by comprising culturing the liver cells in a culture medium containing the test drug in the presence of matrigel and evaluating the ability of the test drug to induce the synthesis of CYP by assaying the enzymatic activity of CYP in the culture medium.

专利号:US-2021062179-A1
优先权日:2015-02-26
标题 :Microsomal bioreactor for synthesis of drug metabolites
发明人：KRISHNAN SADAGOPAN; WALGAMA CHARUKSHA THAMEERA; NERIMETLA RAJASEKHARA REDDY
权利人:UNIV OKLAHOMA STATE
摘要:Reusable microsomal biocatalytic systems (bioreactors) constructed on carbon nanostructure modified electrodes are provided. The bioreactors comprise stable, biologically active immobilized enzymes such as human cytochromes P 450 (CYPs) and their redox partner proteins, e.g. CYP-NADPH (reduced nicotinamide adenine dinucleotide phosphate) reductases (CPR), on the carbon nanostructure surface. The immobilized enzymes may be present in liver microsomes, such as human liver microsomes (HLM) or as bactosomes, S9 fractions, etc. The bioreactors are used, for example, for synthesizing metabolites of interest from compounds such as drugs that are catabolized by the enzymes.

专利号:US-6160006-A
优先权日:1996-10-18
标 题 :6',7'-dihydroxybergamottin, a cytochrome P450 inhibitor in grapefruit
发明人：EDWARDS DAVID J; WOSTER PATRICK M
权利人:UNIV WAYNE STATE
摘要:The present invention provides a composition and methods for inhibiting cytochrome P450 enzyme activity and in particular, inhibiting the activity of the cytochrome P450 3A sub-family of enzymes, specifically, CYP3A4. The present invention provides 6',7'-dihydroxybergamottin, a furanocoumarin, as the compound primarily responsible for the inhibitory effects of grapefruit juice on cytochrome P450 enzyme activity. The present invention also provides a novel synthesis scheme for 6',7'-dihydroxybergamottin.