Category: 1750-45-4

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 1750-45-4, name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, introducing its new discovery. SDS of cas: 1750-45-4

Evaluation of the in vitro/in vivo drug interaction potential of BST204, a purified dry extract of ginseng, and its four bioactive ginsenosides through cytochrome P450 inhibition/induction and UDP-glucuronosyltransferase inhibition

We evaluated the potential of BST204, a purified dry extract of ginseng, to inhibit or induce human liver cytochrome P450 enzymes (CYPs) and UDP-glucuronosyltransferases (UGTs) in vitro to assess its safety. In vitro drug interactions of four bioactive ginsenosides of BST204, S-Rg3, R-Rg3, S-Rh2, and R-Rh2, were also evaluated. We demonstrated that BST204 slightly inhibited CYP2C8, CYP2D6, CYP2C9, and CYP2B6 activities with IC50 values of 17.4, 26.8, 31.5, and 49.7mug/mL, respectively. BST204 also weakly inhibited UGT1A1, UGT1A9, and UGT2B7 activities with IC50 values of 14.5, 26.6, and 31.5mug/mL, respectively. The potential inhibition by BST204 of the three UGT activities might be attributable to S-Rg3, at least in part, as its inhibitory pattern was similar to that of BST204. However, BST204 showed no time-dependent inactivation of the nine CYPs studied. In addition, BST204 did not induce CYP1A2, 2B6, or 3A4/5. On the basis of an in vivo interaction studies, our data strongly suggest that BST204 is unlikely to cause clinically significant drug-drug interactions mediated via inhibition or induction of most CYPs or UGTs involved in drug metabolism in vivo. Our findings offer a clearer understanding and possibility to predict drug-drug interactions for the safe use of BST204 in clinical practice.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. Quality Control of 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 1750-45-4

A cellular model to study drug-induced liver injury in nonalcoholic fatty liver disease: Application to acetaminophen

Obesity and nonalcoholic fatty liver disease (NAFLD) can increase susceptibility to hepatotoxicity induced by some xenobiotics including drugs, but the involved mechanisms are poorly understood. For acetaminophen (APAP), a role of hepatic cytochrome P450 2E1 (CYP2E1) is suspected since the activity of this enzyme is consistently enhanced during NAFLD. The first aim of our study was to set up a cellular model of NAFLD characterized not only by triglyceride accumulation but also by higher CYP2E1 activity. To this end, human HepaRG cells were incubated for one week with stearic acid or oleic acid, in the presence of different concentrations of insulin. Although cellular triglycerides and the expression of lipid-responsive genes were similar with both fatty acids, CYP2E1 activity was significantly increased only by stearic acid. CYP2E1 activity was reduced by insulin and this effect was reproduced in cultured primary human hepatocytes. Next, APAP cytotoxicity was assessed in HepaRG cells with or without lipid accretion and CYP2E1 induction. Experiments with a large range of APAP concentrations showed that the loss of ATP and glutathione was almost always greater in the presence of stearic acid. In cells pretreated with the CYP2E1 inhibitor chlormethiazole, recovery of ATP was significantly higher in the presence of stearate with low (2.5. mM) or high (20. mM) concentrations of APAP. Levels of APAP-glucuronide were significantly enhanced by insulin. Hence, HepaRG cells can be used as a valuable model of NAFLD to unveil important metabolic and hormonal factors which can increase susceptibility to drug-induced hepatotoxicity.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 1750-45-4, name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, introducing its new discovery. SDS of cas: 1750-45-4

In vitro metabolism of magnolol and honokiol in rat liver microsomes and their interactions with seven cytochrome P substrates

Rationale: Magnolol and honokiol are the main active components of Magnolia officinalis Rehd. et Wils. The study of their interactions with liver microsomes is very important for the clinical safety of M. officinalis Rehd. et Wils. Methods: The main metabolites of magnolol and honokiol in rat liver microsomes were investigated using ultrahigh-performance liquid chromatography/mass spectrometry and their possible structures were identified. In addition, cytochrome P450 (CYP450) isoenzymes of the major rat metabolites of magnolol and honokiol were identified using a specific inhibitor. Results: This study suggests that the CYP2E1 subtype is responsible for the oxidation of magnolol and honokiol terminal double bonds to epoxy metabolites. CYP3A4 appears to be the major subtype responsible for further hydrolytic metabolism, while CYP1A2 may promote decarboxylation of the metabolites. CYP2A6 may be the main subtype responsible for the hydrogenation of magnolol (p?< 0.05). Conclusions: This study demonstrated that different CYP450 enzyme isoforms showed different activities in the in vitro metabolism of magnolol and honokiol in rat liver microsomes. It has certain practical applications in that we should pay attention to drug?drug interactions in clinical medications and also to drug?enzyme interactions. We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 1750-45-4, and how the biochemistry of the body works.SDS of cas: 1750-45-4

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Electric Literature of 1750-45-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1750-45-4, Name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, molecular formula is C7H4ClNO3. In a Article£¬once mentioned of 1750-45-4

Validation of LC/MS/MS method for assessment of the in vitro activity of selected rat cytochrome P450 isoenzymes – Application to early drug metabolism screening

A sensitive and specific liquid chromatography/tandem mass spectrometry (LC/MS/MS) method for simultaneous determination of seven metabolites of CYP450 model substrates (acetaminophen, 4-hydroxytolbutamide, 4?-hydroxymephenytoin, 1-hydroxybufuralol, 6-hydroxychlorzoxazone, 1?- and 4?-hydroxymidazolam) in rat liver microsomes was developed. The assay used Kinetex analytical column and a gradient mobile phase consistent of acetonitrile and water with addition of 0.1% formic acid. The analysis was performed in selected reaction monitoring (SRM) mode both in positive and negative (for 6-hydroxychlorzoxazone) mode. The method was validated over the concentration ranges of 10-2000 ng/mL for 4?-hydroxymephenytoin and 4- hydroxytolbutamide, 50-2000 ng/mL for 1-hydroxybufuralol and 25-2000 ng/mL for the rest of the analytes. The intra- and inter-day precision (2-12%) and accuracy (93-119%) were within the limits set by the FDA and EMA guidelines. The developed method was successfully applied to assess the activity of selected CYP450 isoenzymes in rat liver microsomes after addition of ketoconazole.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. Product Details of 1750-45-4, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 1750-45-4

Prediction of cytochrome P450-mediated drug clearance in humans based on the measured activities of selected CYPs

Determining drug-metabolizing enzyme activities on an individual basis is an important component of personalized medicine, and cytochrome P450 enzymes (CYPs) play a principal role in hepatic drug metabolism. Herein, a simple method for predicting the major CYP-mediated drug clearance in vitro and in vivo is presented. Ten CYP-mediated drug metabolic activities in human liver microsomes (HLMs) from 105 normal liver samples were determined. The descriptive models for predicting the activities of these CYPs in HLMs were developed solely on the basis of the measured activities of a smaller number of more readily assayed CYPs. The descriptive models then were combined with the Conventional Bias Corrected in vitro-in vivo extrapolation method to extrapolate drug clearance in vivo. The Vmax, Km, and CLint of six CYPs (CYP2A6, 2C8, 2D6, 2E1, and 3A4/5) could be predicted by measuring the activities of four CYPs (CYP1A2, 2B6, 2C9, and 2C19) in HLMs. Based on the predicted CLint, the values of CYP2A6-, 2C8-, 2D6-, 2E1-, and 3A4/5-mediated drug clearance in vivo were extrapolated and found that the values for all five drugs were close to the observed clearance in vivo. The percentage of extrapolated values of clearance in vivo which fell within 2-fold of the observed clearance ranged from 75.2% to 98.1%. These findings suggest that measuring the activity of CYP1A2, 2B6, 2C9, and 2C19 allowed us to accurately predict CYP2A6-, 2C8-, 2D6-, 2E1-, and 3A4/5-mediated activities in vitro and in vivo and may possibly be helpful for the assessment of an individual’s drug metabolic profile.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. Recommanded Product: 1750-45-4, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 1750-45-4

Molecular simulation of nonfacilitated membrane permeation

This is a review. Non-electrolytic compounds typically cross cell membranes by passive diffusion. The rate of permeation is dependent on the chemical properties of the solute and the composition of the lipid bilayer membrane. Predicting the permeability coefficient of a solute is important in pharmaceutical chemistry and toxicology. Molecular simulation has proven to be a valuable tool for modeling permeation of solutes through a lipid bilayer. In particular, the solubility-diffusion model has allowed for the quantitative calculation of permeability coefficients. The underlying theory and computational methods used to calculate membrane permeability are reviewed. We also discuss applications of these methods to examine the permeability of solutes and the effect of membrane composition on permeability. The application of coarse grain and polarizable models is discussed. This article is part of a Special Issue entitled: Membrane Proteins edited by J.C. Gumbart and Sergei Noskov.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1750-45-4, Name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, belongs to benzoxazole compound, is a common compound. Computed Properties of C7H4ClNO3In an article, once mentioned the new application about 1750-45-4.

Obesity-induced increase of CYP2E1 activity and its effect on disposition kinetics of chlorzoxazone in Zucker rats

This study was designed to investigate the induction of CYP2E1 in obese Zucker rats and its effect on the disposition kinetics of chlorzoxazone (CZX). CZX 20 mg/kg was administered to three groups of rats: normal Zucker rats fed a normal diet (ND), normal Zucker rats fed a high-fat diet (HF), and genetically obese Zucker rats fed a normal diet (OB). The values of the area under the plasma concentration-time curve from 0 to ? (AUC?) of CZX were in the order of ND > HF > OB rats. The AUC? values of total 6-hydroxychlorzoxazone (6OHCZX-T), which is considered to be a CYP2E1 metabolic marker, were in the opposite order. The values of the AUC? ratio (6OHCZX-T/CZX) in ND, HF and OB rats were approximately 0.2, 0.3 and 0.4, respectively. The CZX concentration in fat was much higher than the concentrations in plasma, liver and kidney in all groups. Induction of CYP2E1 protein was greater in both liver and fat of OB rats than in those of HF rats. Microsomal activity of CYP2E1 in liver and fat was also in the order of OB > HF > NM rats. These results suggest that CYP2E1 may be induced in liver and fat of obese patients, thereby potentially altering the disposition kinetics of not only CZX, but also other lipophilic drugs metabolized by CYP2E1.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 1750-45-4, name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, introducing its new discovery. name: 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one

NEW LOW SIDE EFFECT PHARMACEUTICAL COMPOSITION CONTAINING ANTITUBERCULOSIS DRUGS

A pharmaceutical composition for treating tuberculotic diseases with no side effect/low side effect is provided by the present invention, which pharmaceutically effective amount of one or more compounds chosen from isoniazid, rifampin, pyrazinamide and ethambutol, and pharmaceutically effective amount of substances which can reduce the side effect of the antituberculosis agents.

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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, Recommanded Product: 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

Effects of honokiol on CYP450 activity and transporter mRNA expression in type 2 diabetic rats

This study was aimed to clarify the effect of honokiol (Hon) on the activity of Cytochrome P450 (CYP450) enzymes, and the level of mRNA expression of liver and kidney transporters in type 2 diabetic rats induced by high-fat diet and strepotozotocin. Rats were randomly divided into normal control (NC) group, diabetic control (DC) group and Hon groups (n = 6). The activities of hepatic CYP1A2, CYP2E1, CYP2C, CYP2B, CYP3A and CYP4A, and the mRNA expression levels of hepatic and renal transporters, were determined. Compared to the NC group, the activities of CYP1A2, CYP2E1, CYP4A and CYP2C in DC group were increased by 2.36-, 2.10-, 2.55- and 1.86-fold, respectively. The mRNA expression levels of hepatic Oat2, Oatp2b1 and Oatp1a5, and renal Oct1, Octn2, Oatp2b1 and Oatp1a5, were significantly down-regulated, while the mRNA expression levels of hepatic Octn2, Oatp3a1, Oatp1a1 and Mdr2, and renal Oat2, Mrp4 and Bcrp, were significantly upregulated. Compared to the DC group, Hon treatment significantly inhibited the activity of hepatic CYP2E1, CYP4A, 3A and CYP1A2 by 45.6%, 29.2%, 22.7% and 20.7% in Hon high dose group, respectively. Moreover, Hon treatment significantly inhibited the mRNA expression levels of renal Bcrp and Mrp4 by 2.63-fold and 1.54-fold, while significantly upregulated the mRNA expression levels of hepatic Oat2 and Oatp2b1 by 1.52-fold and 1.54-fold in Hon high dose group, respectively. The results suggested that under the diabetes condition, the changes of CYP450 activity and transporter expression inevitably interfere the normal transport, metabolism and efficacy of drugs. The present work firstly reported that Hon treatment ameliorated the abnormal change of hepatic CYP activity (including CYP2E1, CYP4A and CYP1A2) and the transporter mRNA expression (including hepatic Oat2 and Oatp2b1, renal Bcrp and Mrp4) in type 2 diabetic rats induced by high-fat diet and strepotozotocin, which are associated with the occurrence and development of diabetes.

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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. COA of Formula: C7H4ClNO3. Introducing a new discovery about 1750-45-4, Name is 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one

Impaired 6-hydroxychlorzoxazone elimination in patients with kidney disease: Implication for cytochrome P450 2E1 pharmacogenetic studies

Objective: The purposes of this study were (1) to describe the disposition of chlorzoxazone and 6-hydroxychlorzoxazone in patients with kidney disease, (2) to develop a population pharmacokinetic model including covariates that may influence the pharmacokinetic variability of both compounds, and (3) to examine the effect of covariates on the chlorzoxazone metabolic ratio. Methods: Twenty-one subjects received a single oral dose of chlorzoxazone, 250 mg, and plasma and urine samples were collected for up to 120 hours. The impact of creatinine clearance (CLcr), age, and weight on chlorzoxazone and 6-hydroxychlorzoxazone clearance terms was assessed with NONMEM software (v.5, level 1.1; Globomax LLC, Hanover, Md) by use of a stepwise backward-elimination technique and the likelihood ratio test. Results: A linear model with first-order absorption for chlorzoxazone and first-order formation for 6-hydroxychlorzoxazone simultaneously described the disposition of both compounds. Weight was a significant predictor of 6-hydroxychlorzoxazone formation clearance and other, unaccounted for clearance of chlorzoxazone, whereas CLcr was a significant predictor of 6-hydroxychlorzoxazone renal clearance. No relationship between CLcr. and formation clearance was observed. The 6-hydroxychlorzoxazone area under the plasma concentration-time curve was inversely related to CLcr, even within the range of normal renal function, resulting in chlorzoxazone metabolic ratio values that were substantially higher in subjects with kidney disease. Both the experimental data and model-based Monte Carlo simulations revealed greatly increased chlorzoxazone metabolic ratio values when CLcr was low and weight was high. Conclusions: Although cytochrome P450 (CYP) 2E1 activity, as estimated by 6-hydroxychlorzoxazone formation clearance, was not affected by kidney disease, the chlorzoxazone metabolic ratio was substantially elevated in these subjects. The results of this study show that the commonly used plasma-based chlorzoxazone metabolic ratio is dependent on renal function and, therefore, does not provide a reliable index of CYP2E1-mediated metabolism.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem