7-乙氧基-4-(三氟甲基)香豆素
7-乙氧基-4-(三氟甲基)香豆素结构式
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常用名 | 7-乙氧基-4-(三氟甲基)香豆素 | 英文名 | 7-Ethoxy-4-(trifluoromethyl)coumarin |
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| CAS号 | 115453-82-2 | 分子量 | 258.19300 | |
| 密度 | 1.368 g/cm3 | 沸点 | 303.1ºC at 760 mmHg | |
| 分子式 | C12H9F3O3 | 熔点 | N/A | |
| MSDS | 中文版 美版 | 闪点 | 132.7ºC |
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HepG2 cells as an in vitro model for evaluation of cytochrome P450 induction by xenobiotics.
Arch. Pharm. Res. 38 , 691-704, (2015) Although various in vitro assays have been developed to evaluate the cytochrome P450 (CYP)-inducing potential of drug candidates, there is a continuing need for the development of a reliable model in drug discovery. The objective of the present study was to c... |
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Environmentally persistent free radical-containing particulate matter competitively inhibits metabolism by cytochrome P450 1A2.
Toxicol. Appl. Pharmacol. 289 , 223-30, (2015) Combustion processes generate different types of particulate matter (PM) that can have deleterious effects on the pulmonary and cardiovascular systems. Environmentally persistent free radicals (EPFRs) represent a type of particulate matter that is generated a... |
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Inhibition of cytochrome P450 2B4 by environmentally persistent free radical-containing particulate matter.
Biochem. Pharmacol. 95 , 126-32, (2015) Combustion processes generate particulate matter (PM) that can affect human health. The presence of redox-active metals and aromatic hydrocarbons in the post-combustion regions results in the formation of air-stable, environmentally persistent free radicals (... |
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Effects of artemisinin antimalarials on Cytochrome P450 enzymes in vitro using recombinant enzymes and human liver microsomes: potential implications for combination therapies.
Xenobiotica 44(7) , 615-26, (2014) 1. Cytochrome P450 enzyme system is the most important contributor to oxidative metabolism of drugs. Modification, and more specifically inhibition, of this system is an important determinant of several drug-drug interactions (DDIs). 2. Effects of the antimal... |
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Interaction of selected platinum(II) complexes containing roscovitine-based CDK inhibitors as ligands with human liver microsomal cytochrome P450.
Biomed. Pap. Med. Fac. Univ. Palacky. Olomouc. Czech. Repub. 159 , 382-7, (2015) We studied the interaction of oxaliplatin derivatives involving cytotoxic adenine-based cyclin-dependent kinase inhibitors, with human liver microsomal cytochrome P450.The activities of 9 human liver microsomal CYP forms (CYPs 1A2, 7-ethoxyresorufin O-deethyl... |
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Re-engineering cytochrome P450 2B11dH for enhanced metabolism of several substrates including the anti-cancer prodrugs cyclophosphamide and ifosfamide.
Arch. Biochem. Biophys. 458(2) , 167-74, (2007) Based on recent directed evolution of P450 2B1, six P450 2B11 mutants at three positions were created in an N-terminal modified construct termed P450 2B11dH and characterized for enzyme catalysis using five substrates. Mutant I209A demonstrated a 3.2-fold enh... |
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Mutagenesis and molecular dynamics suggest structural and functional roles for residues in the N-terminal portion of the cytochrome P450 2B1 I helix.
Arch. Biochem. Biophys. 423(2) , 266-76, (2004) To investigate their potential roles in ligand access, binding, and subsequent metabolism, residues in the N-terminal portion of the cytochrome P450 2B1 I helix were mutated to alanine and phenylalanine. Of the 18 mutants from E286 to S294 only 7 yielded holo... |
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Mechanism-Based Inactivation of Human Cytochrome P450 2B6 by Chlorpyrifos.
Chem. Res. Toxicol. 28 , 1484-95, (2015) Chlorpyrifos (CPS) is a commonly used pesticide which is metabolized by P450s into the toxic metabolite chlorpyrifos-oxon (CPO). Metabolism also results in the release of sulfur, which has been suggested to be involved in mechanism-based inactivation (MBI) of... |
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Investigation of the role of cytochrome P450 2B4 active site residues in substrate metabolism based on crystal structures of the ligand-bound enzyme.
Arch. Biochem. Biophys. 455(1) , 61-7, (2006) Based on the X-ray crystal structures of 4-(4-chlorophenyl)imidazole (4-CPI)- and bifonazole (BIF)-bound P450 2B4, eight active site mutants at six positions were created in an N-terminal modified construct termed 2B4dH and characterized for enzyme inhibition... |
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Structure-activity relationship and elucidation of the determinant factor(s) responsible for the mechanism-based inactivation of cytochrome P450 2B6 by substituted phenyl diaziridines.
Drug Metab. Dispos. 34(12) , 2102-10, (2006) It has been demonstrated previously that several 3-trifluoromethyl-3-(4-alkoxyphenyl)diaziridines inhibit the 7-ethoxy-4-(trifluoroethyl)coumarin (7-EFC) O-deethylation activity of P450 2B6 in a mechanism-based manner. In contrast, 3-trifluoromethyl-3-(4-meth... |