Category: 1750-45-4

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The effect of broccoli in diet on the cytochrome P450 activities of tilapia fish (Oreochromis niloticus) during phenol exposure

Aquaculture is the fastest growing animal food-producing sector and represents around 40% of global fish production. Doubtless, aquaculture will be soon the main world source of marine and freshwater food, over the capture fishery. Water pollution is a main concern for production and represents a public health risk. Cruciferous vegetables, as broccoli, have been reported to have a chemoprotection capacity against the effect of pollutants on different organisms. Broccoli and its phytochemicals are able to modulate the cytochrome P450 enzymes (CYP) which are involved in the xenobiotic metabolism. In this work, the effect of a broccoli-rich diet on different cytochromes P450 activities in liver from tilapia juveniles exposed to phenol was determined. Activities on phenacetin, chlorzoxazone, tolbutamide, mephenytoin, dextromethorphan, and testosterone, were monitored in tilapia liver extracts from fish fed with and without enriched broccoli diets, before and after phenol exposure. Fish were fed with broccoli and control diets during 30 days prior to phenol exposure at two sub-lethal concentrations of phenol (2 and 20 mg L-1), then the profile of CYP activities was determined at 0, 12 and 24 h after phenol addition. Before phenol addition fish fed with broccoli-rich diet showed a significant induction of phenacetin and tolbutamide activities when compared with liver extracts from fish fed with control diet. After phenol exposure a clear and steady induction of the dextromethorphan and mephenytoin activities were detected. In spite of the fact that substrates are not specific for each CYP, the increase of activity on dextromethorphan could represent the first report of a hepatic CYP2D6 induction by the presence of a xenobiotic. In addition, phenol exposure through diet was evaluated. Consistently with the previous experiments, phenacetin and chlorzoxazone showed higher activities while dextromethorphan and testosterone activities were lower in the liver extract from fish fed with broccoli than in control fish. Interestingly, tolbutamide activity was significantly higher in fish fed with broccoli than these observed in the controls, while mephenytoin showed 8-times higher activity in fish fed with control diet than those fed with broccoli enriched diet. The role of cytochrome P450 enzymes in the xenobiotic metabolism and the potential use of designed diets, containing chemoprotectors, to contend against pollutant effects on cultivated fish are discussed.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Synthetic Route of 1750-45-4, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 1750-45-4, 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, introducing its new discovery.

Ultrasensitive quantification of the CYP2E1 probe chlorzoxazone and its main metabolite 6-hydroxychlorzoxazone in human plasma using ultra performance liquid chromatography coupled to tandem mass spectrometry after chlorzoxazone microdosing

Chlorzoxazone is a probe drug to assess cytochrome P450 (CYP) 2E1 activity (phenotyping). If the pharmacokinetics of the probe drug is linear, pharmacologically ineffective doses are sufficient for the purpose of phenotyping and adverse effects can thus be avoided. For this reason, we developed and validated an assay for the ultrasensitive quantification of chlorzoxazone and 6-hydroxychlorzoxazone in human plasma. Plasma (0.5 mL) and liquid/liquid partitioning were used for sample preparation. Extraction recoveries ranged between 76 and 93% for both analytes. Extracts were separated within 3 min on a Waters BEH C18 Shield 1.7 mum UPLC column with a fast gradient consisting of aqueous formic acid and acetonitrile. Quantification was achieved using internal standards labeled with deuterium or 13C and tandem mass spectrometry in the multiple reaction monitoring mode using negative electrospray ionization, which yielded lower limits of quantification of 2.5 pg mL-1, while maintaining a precision always below 15%. The calibrated concentration ranges were linear for both analytes (2.5-1000 pg mL-1) with correlation coefficients of >0.99. Within-batch and batch-to-batch precision in the calibrated ranges for both analytes were <15% and <11% and plasma matrix effects always were below 50%. The assay was successfully applied to assess the pharmacokinetics of chlorzoxazone in two human volunteers after administration of single oral doses (2.5-5000 mug). This ultrasensitive assay allowed the determination of chlorzoxazone pharmacokinetics for 8 h after microdosing of 25 mug chlorzoxazone. Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 1750-45-4. In my other articles, you can also check out more blogs about 1750-45-4

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. HPLC of Formula: C7H4ClNO3. Introducing a new discovery about 1750-45-4, Name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one

Timing in drug absorption and disposition: The past, present, and future of chronopharmacokinetics

The importance of drug dosing time in pharmacokinetics, pharmacodynamics, and toxicity is receiving increasing attention from the scientific community. In spite of mounting evidence that circadian oscillations affect drug absorption, distribution, metabolism, and excretion (ADME), there remain many unanswered questions in this field and, occasionally, conflicting experimental results. Such data arise not only from translational difficulties caused by interspecies differences but also from variability in study design and a lack of understanding of how the circadian clock affects physiological factors that strongly influence ADME, namely, the expression and activity of drug transporters. Hence, the main goal of this review is to provide an updated analysis of the role of the circadian rhythm in drug absorption, distribution across blood?tissue barriers, metabolism in hepatic and extra-hepatic tissues, and hepatobiliary and renal excretion. It is expected that the research suggestions proposed here will contribute to a tissue-targeted and time-targeted pharmacotherapy.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Quality Control of 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 1750-45-4, Name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, molecular formula is C7H4ClNO3

mRNA transfection retrofits cell-based assays with xenobiotic metabolism

The US EPA’s ToxCast program is designed to assess chemical perturbations of molecular and cellular endpoints using a variety of high-throughput screening (HTS) assays. However, existing HTS assays have limited or no xenobiotic metabolism which could lead to false positive (chemical is detoxified in vivo) as well as false negative results (chemical is bioactivated in vivo) and thus potential mischaracterization of chemical hazard. To address this challenge, the ten most prevalent human liver cytochrome P450 (CYP) enzymes were introduced into a human cell line (HEK293T) with low endogenous metabolic capacity. The CYP enzymes were introduced via transfection of modified mRNAs as either singlets or as a mixture in relative proportions as expressed in human liver. Initial experiments using luminogenic substrates demonstrate that CYP enzyme activities are significantly increased when co-transfected with an mRNA encoding a CYP accessory protein, P450 oxidoreductase (POR). Transfected HEK293T cells demonstrate the ability to produce predicted metabolites following treatment with well-studied CYP substrates for at least 18 h post-treatment. As a demonstration of how this method can be used to retrofit existing HTS assays, a proof-of-concept screen for cytotoxicity in HEK293T cells was conducted using 56 test compounds. The results demonstrate that the xenobiotic metabolism conferred by transfection of CYP-encoding mRNAs shifts the dose-response relationship for some of the tested chemicals such as aflatoxin B1 (bioactivation) and fenazaquin (detoxification). Overall, transfection of CYP-encoding mRNAs is an effective and portable solution for retrofitting existing cell-based HTS assays with metabolic competence.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Application In Synthesis of 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 1750-45-4, name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one. In an article£¬Which mentioned a new discovery about 1750-45-4

Dose-response of oridonin on hepatic cytochromes P450 mRNA expression and activities in mice

ETHNOPHARMACOLOGICAL RELEVANCE: Oridonin, the major terpene found in Rabdosia rubescens, is widely used as a dietary supplement or therapeutic drug. The effects of oridonin on drug processing genes, such as cytochrome P450 and nuclear receptors, were still unclear. Therefore, the present study investigated the influence of oridonin on the hepatic drug metabolizing system to evaluate the safety through its drug interaction potential.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Computed Properties of C7H4ClNO3, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 1750-45-4, name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one. In an article£¬Which mentioned a new discovery about 1750-45-4

The inhibition of major human hepatic cytochrome P450 enzymes by 18 pesticides: Comparison of the N-in-one and single substrate approaches

In the present study on human hepatic microsomes, the N-in-one assay with ten probe substrates for nine cytochrome-P450 enzymes (CYPs) was compared with the single substrate assays to investigate pesticides-CYP interactions. CYP inhibition was measured by liquid chromatography-tandem mass spectrometry (LC/MS-MS). As illustrated by the initial screening at 100muM concentration of 18 pesticides, CYPs are more sensitive to organophosphates (OPs) than to other pesticide groups. Chlorpyrifos and fenitrothion were most effective in inhibiting CYP1A1/2, and CYP2B6. Profenofos was also inhibitory towards multiple CYPs. Pyrethroids, e.g. deltamethrin, fenvalerate and lambda-cyhalothrin, potently inhibited CYP2D6. CYP3A4 activity was moderately inhibited by fenvalerate and potently by alpha-cypermethrin. The correlations between IC50 values obtained from the N-in-one and single substrate approaches were highly significant for CYP2Cs (r2=0.94), CYP3A4, omeprazole-sulfoxidation, (r2=0.89), followed by CYP1A2 and CYP2B6 (r2=0.82), and CYP2D6 (r2=0.80). In contrast no correlation was observed with CYP2E1 and CYP3A4 (midazolam-1′-hydroxylation). The N-in-one screening assay seems useful and reliable for most CYP activities when a comprehensive and quick evaluation of potential interactions with CYPs is needed. However, at the present moment, it does not enable discrimination on the basis of mechanism of inhibition. A strict comparison between single and N-in-one assays is a prerequisite for more extensive routine use.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 1750-45-4, help many people in the next few years.Computed Properties of C7H4ClNO3

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. name: 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one. Introducing a new discovery about 1750-45-4, Name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one

In vitro inhibitory effects of esculetin on human liver cytochrome P450 enzymes

Esculetin (ESC), a derivative of coumarin, possesses a number of pharmacological activities. Cytochrome P450 (CYP) enzymes play a vital role in the biotransformation of xenobiotics; its activity di-rectly affects the bioavailability of the drugs. Therefore, should be paid attention in the effect of ESC on the activity of CYPs. The effects of ESC on eight human liver CYP isoforms (i.e., 1A2, 3A4, 2A6, 2E1, 2D6, 2C9, 2C19 and 2C8) were investigated in vitro using human liver microsomes (HLMs), and the enzyme kinetic parameters were calculated. ESC inhibited the activity of CYP3A4, CYP2E1 and CYP1A2, with IC50 values of 15.01, 23.22 and 19.42 muM, respectively, but other CYPs were not affected. The inhibition of CYP3A4 by ESC was best fitted in a non-competitive manner, with the Ki value of 7.53 muM. Whereas, ESC competitively inhibited the activity of CYP2E1 and CYP1A2, with Ki values of 11.13 and 9.19 muM, re-spectively. In addition, ESC is a time dependent inhibitor for CYP3A4 with KI/Kinact value of 9.52/0.061 min?1muM?1. The in vitro studies of ESC with CYP isoforms indicate that ESC has the potential to cause pharmacokinetic drug interactions with other co-administered drugs metabolized by CYP3A4, CYP2E1 and CYP1A2. Further clinical studies are needed to evaluate the significance of this interaction.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Related Products of 1750-45-4, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 1750-45-4, molcular formula is C7H4ClNO3, introducing its new discovery.

Marmoset pulmonary cytochrome P450 2F1 oxidizes biphenyl and 7-ethoxycoumarin and hepatic human P450 substrates

1. A potentially useful animal model for preclinical studies is the common marmoset (Callithrix jacchus). In this study, using reverse-transcription polymerase chain reaction from marmoset livers, we identified a novel cytochrome P450 (P450) 2F1 cDNA with an open reading frame of 1473 bp. 2. High sequence identities of 92-94% with primate P450 2 F amino acid sequences were indicated by deduced amino acid sequences of P450 2F1 cDNA. Phylogenetic analysis indicates that marmoset P450 2F1 is more congruent with primate P450 2 F forms than those of other species such as rodents. 3. Among five tissue types examined, abundant expression of marmoset P450 2F1 mRNA and P450 2F1 protein in lungs was shown. Cynomolgus monkey P450 2F1 mRNA was abundantly expressed in lungs as well as testes and ovaries in 10 tissue types. 4. Similar to those of humans and cynomolgus monkeys, marmoset P450 2F1 heterologously expressed in Escherichia coli membranes efficiently catalyzed 7-ethoxycoumarin O-deethylation and biphenyl hydroxylation, however unlike human P450 2F1, marmoset P450 2F1 exhibited hydroxylation activity toward coumarin and chlorzoxazone. 5. These findings indicated that P450 2F1 enzyme expressed in marmoset lungs and also catalyzed metabolism of xenobiotics, suggesting the importance of P450 2 F-dependent drug metabolism in marmoset lungs.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 1750-45-4 is helpful to your research. Related Products of 1750-45-4

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Safety of 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 1750-45-4, Name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, molecular formula is C7H4ClNO3

Multifaceted interaction of the traditional Chinese medicinal herb Schisandra chinensis with cytochrome P450-mediated drug metabolism in rats

ETHNOPHARMACOLOGICAL RELEVANCE: Schisandra chinensis (SC), officially listed as a sedative and tonic in the Chinese Pharmacopoeia, has been used as a common component in various prescriptions in Traditional Chinese Medicine (TCM) and more recently in western medicine for its antihepatotoxic effect. To assess the possible herb-drug interaction, effects of SC extracts on hepatic cytochrome P450 (P450, CYP) enzymes were studied.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Safety of 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 1750-45-4, in my other articles.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 1750-45-4, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 1750-45-4, name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one. In an article£¬Which mentioned a new discovery about 1750-45-4

Stereoselective interaction between tetrahydropalmatine enantiomers and CYP enzymes in human liver microsomes

Tetrahydropalmatine (THP), with one chiral center, is an alkaloid that possesses analgesic and many other pharmacological actives. The aim of the present study is to investigate stereoselective metabolism of THP enantiomers in human liver microsomes (HLM) and elucidate which cytochrome P450 (CYP) isoforms contribute to the stereoselective metabolism in HLM. Additionally, the inhibitions of THP enantiomers on activity of CYP enzymes are also investigated. The results demonstrated that (+)-THP was preferentially metabolized by HLM. Ketoconazole (inhibitor of CYP3A4/5) inhibited metabolism of (-)-THP or (+)-THP at same degree, whereas the inhibition of fluvoxamine (inhibitor of CYP1A2) on metabolism of (+)-THP was greater than that of (-)-THP; moreover, the metabolic rate of (+)-THP was 5.3-fold of (-)-THP in recombinant human CYP1A2. Meanwhile, THP enantiomers did not show obvious inhibitory effect on the activity of various CYP isoforms (CYP1A2, 2A6, 2C8, 2C9, 2C19, 2E1, and 3A4/5), whereas (-)-THP, but not (+)-THP, significantly inhibited the activity of CYP2D6 with the Ki value of 6.42 ¡À 0.38 muM. The results suggested that THP enantiomers were predominantly metabolized by CYP3A4/5 and CYP1A2 in HLM, and (+)-THP was preferentially metabolized by CYP1A2, whereas CYP3A4/5 contributed equally to metabolism of (-)-THP or (+)-THP. Besides, the inhibition of CYP2D6 by (-)-THP may cause drug-drug interaction, which should be considered. Copyright

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem