Category: 125995-03-1

You could be based in a university, combining chemical research with teaching; in a pharmaceutical company, working on developing and trialing new drugs; helping to ensure national healthcare provision keeps pace with new discoveries. 125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Article，once mentioned of 125995-03-1, Application In Synthesis of Atorvastatin lactone

The cholesterol-reducing drug atorvastatin is widely used in hyperlipidemic patients and it is crucial to consider its potential myotoxic effect when adjusting the prescription for patients. The aim of this study was to establish a simple high-performance liquid chromatography method that would be applicable for the quantitative determination of high serum atorvastatin concentrations in patients for the assessment of myalgia. The average recovery of atorvastatin from the extraction using ethyl acetate was 85.1%. The extract was dried, re-dissolved in methanol, and subjected to chromatographic separation using a reverse-phase C18 analytical column and a mobile phase consisting of 61.3% methanol in 0.05 M sodium phosphate buffer at pH 3.5. The concentration of atorvastatin was quantitatively determined by measuring the absorbance at 247 nm and beta-naphthoflavone was used as an internal standard. The lower limits of detection and quantification of atorvastatin were 1.2 ng/mL and 3.0 ng/mL, respectively. There was a good linear relationship (r = 0.999) of the peak area and atorvastatin within a concentration range of 3.0-150 ng/mL in human serum. Among 61 lipid-controlling patients with detectable serum atorvastatin concentrations, 7 patients had myalgia and their serum concentrations were not significantly greater than those in patients without myalgia. Copyright

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Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals. However, they have proven to be challenging because of the mutual inactivation of both catalysts. 125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Article，once mentioned of 125995-03-1, Related Products of 125995-03-1

1. We investigated the structure-activity relationship of 31 kinds of synthesized atorvastatin esters, thioesters, amides and lactone, selected as prodrug models, for metabolic activation by microsomes and hydrolases. 2. The susceptibility to human carboxylesterase 1 (hCES1) was influenced not only by the size of the acyl group and alkoxy group but also by the degree of steric crowding around the alkoxy group. 3. The susceptibility to human carboxylesterase 2 (hCES2) increased with a decrease in electron density around the alkoxy group of the substrate. 4. Lactone was specifically hydrolyzed by paraoxonase 3 (PON3). 5. These findings should be useful in prodrug design for controlling metabolic activation.

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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. 125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Chapter，once mentioned of 125995-03-1, Safety of Atorvastatin lactone

The development of synthetic routes to atorvastatin, probably the most commercially successful small molecule drug ever launched, has spanned some 25 years. The changing requirements of synthetic routes and the reagents encompassed by these have paralleled the life-cycle of the drug. These requirements have shifted from flexibility, reliability and speed in the medicinal chemistry phase to suitability for scale-up and overall yield in the development phase. Emphasis on routes that exhibit low cost and reduced environmental impact has come to the forefront in manufacturing. The desire for increasingly efficient and low-hazard chemistry in the development and manufacture of this drug has been both accompanied by and provided a stimulus to the rise of asymmetric catalysis, especially biocatalysis. The implementation of asymmetric catalysis, and its integration into the overall route alongside other improvements has had a major impact in increased efficiency and minimisation of hazards in production of this drug.

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Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn’t involve a screen. 125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Patent，once mentioned of 125995-03-1, Recommanded Product: 125995-03-1

This invention provides a new method for the preparation of statins comprising hydrolyzing a mixture of compounds of the following formulas (Formula III and IV).

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Chemical research careers are more diverse than they might first appear, as there are many different reasons to conduct research and many possible environments. Introducing a new discovery about 125995-03-1, Name is Atorvastatin lactone, HPLC of Formula: C33H33FN2O4.

The statins are widely used worldwide to reduce risk for cardiovascular events in both the primary and secondary prevention settings. Although generally quite safe, the statins can be associated with a variety of serious side adverse effects, including myalgia, myopathy, and changes in plasma enzymes of hepatic origin. Although rare, the most serious of these is rhabdomyolysis. Several drugs can interfere with the metabolism and disposal of the statins, thereby increasing risk for adverse events. It is important that clinicians treating patients with statins be aware of the potential for drug-drug interactions between each statin and specific other drugs and take measures to prevent them. The prediction of potential drug-drug interactions derives from basic pharmacokinetic principles. Certain drug interactions are predicted by measuring the effect of interacting drugs on blood plasma concentrations of the statin. Individual patient variations resulting in part from polymorphisms in the metabolizing enzymes confound some of these predictions. Based on these known effects, a new classification for predicting statin drug interactions is proposed. This report discusses likely prescription and nonprescription interactions as well as potential alternatives for special populations. Published by Elsevier Inc. on behalf of National Lipid Association.

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The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. 125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Review，once mentioned of 125995-03-1, HPLC of Formula: C33H33FN2O4

Pollution by Organic Contaminants (OC) in aquatic environments is a relevant issue at the global scale. Lipids comprised of Fatty Acids (FA) play many important roles in the physiology and life history of fishes. Toxic effects of OC are partly dependent on its bioaccumulation in the lipids of aquatic organisms due its physicochemical properties. Therefore, there is an increasing interest to investigate the gene expression as well as the presence and activity of proteins involved in FA metabolism. The attention on Peroxisome Proliferation Activate Receptors (PPARs) also prevails in fish species exposed to OC and in the transport, biosynthesis and beta-oxidation of FA. Several studies have been conducted under controlled conditions to evaluate these biological aspects of fish species exposed to OC, as fibrates, endocrine disrupting compounds, perfluoroalkyl acids, flame retardants, metals and mixtures of organic compounds associated with a polluted area. However, only fibrates, which are agonists of PPARs, induce biological responses suitable to be considered as biomarkers of exposure to these pollutants. According to the documented findings on this topic, it is unlikely that these physiological aspects are suitable to be employed as biomarkers with some noticeable exceptions, which depend on experimental design. This emphasises the need to investigate the responses in fish treated with mixtures of OC and in wild fish species from polluted areas to validate or refute the suitability of these biomarkers for environmental or fish health monitoring.

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Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. In an article, published in an article, once mentioned the application of 125995-03-1, Name is Atorvastatin lactone,molecular formula is C33H33FN2O4, is a conventional compound. this article was the specific content is as follows.SDS of cas: 125995-03-1

The present invention relates to a process for preparing C7 intermediates and their use in the preparation of pyrrole derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, and more particularly to improved synthetic methods for preparing 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids. The invention further relates to intermediates in this process.

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name: Atorvastatin lactone, Some examples of the diverse research done by chemistry experts include discovery of new medicines and vaccines, improving understanding of environmental issues, and development of new chemical products and materials. An article , which mentions 125995-03-1, molecular formula is C33H33FN2O4. The compound – Atorvastatin lactone played an important role in people’s production and life.

Statins are effective drugs to reduce cardiovascular events secondary to dyslipidemia; however, they cause frequent undesirable side effects. The incidence of statin-induced myotoxicity (SIM) is presented by 7 to 29% of patients, depending upon the report. SIM may develop in presence of abnormally high concentrations of statins in the myocyte and/or in presence of muscular conditions that may predispose to SIM. High concentrations of statins in the myocyte may occur whenever the activity of liver influx membrane transporters, namely OATP1B1, of drug metabolizing enzymes, and of liver and muscular efflux transporters, MDR1 and BCRP, is reduced. In the muscle, conditions that may predispose to SIM include mitochondrial damage with disruption of the mitochondrial respiratory chain and decreased production of ATP, increase of ROS, and leak of cytochrome c and Ca2 +. In the sarcoplasma, statins activate MAPK and diminish the RhoA/AKT/mTOR/PGC-1alpha pathway. All these effects contribute to activate apoptosis, proteolysis, and muscle remodeling. Moreover, in the sarcoplasma, statins can reduce the resting chloride channel conductance, as well as lactate efflux. These changes will be responsible of fatigue, cramps, myalgia and elevation of serum CK. To date, besides avoiding drug-drug interactions and alcohol consumption, and correcting hypothyroidism, two strategies could be useful to prevent/diminish SIM, e.g. gradual dose titration with statins less prone to produce SIM, and high supplements of vitamin D in subjects with low plasma concentrations of 25(OH) D3.

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Electric Literature of 125995-03-1. Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Like 125995-03-1, Name is Atorvastatin lactone. In a document type is Article, introducing its new discovery.

Pravastatin is a well known 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor. Cumulative studies have shown that pravastatin is taken up into hepatocytes by the organic anion transporting polypeptide family transporters and excreted into the bile as an intact form by multidrug resistance-associated protein 2 (MRP2). It is generally accepted that the bile salt export pump (BSEP/ABCB11) mainly transports bile acids and plays an indispensable role in their biliary excretion. Interestingly, we found that BSEP could accept pravastatin as a substrate. Significant ATP-dependent uptake of pravastatin by human BSEP (hBSEP)- and rat BSEP (rBsep)-expressing membrane vesicles was observed, and the ratio of the uptake activity of pravastatin to that of taurocholic acid (TCA) by hBSEP was 3.3-fold higher than that by rBsep. The Km value of pravastatin for hBSEP was 124 muM. A mutual inhibition study between TCA and pravastatin revealed that they competitively interact with hBSEP. Several statins inhibited the hBSEP- and rBsep-mediated uptake of TCA; however, the specific uptake of other statins (cerivastatin, fluvastatin, and pitavastatin) by hBSEP and rBSEP was not detected. The inhibitory effects of hydrophilic statins (pravastatin and rosuvastatin) on the uptake of TCA by BSEP were relatively lower than those of lipophilic statins. These data suggest that BSEP may be partly involved in the biliary excretion of pravastatin in both rats and humans. Copyright

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HPLC of Formula: C33H33FN2O4. Healthcare careers for chemists are once again largely based in laboratories, although increasingly there is opportunity to work at the point of care, helping with patient investigation. 125995-03-1, Name is Atorvastatin lactone. In a document type is Article, introducing its new discovery.

Atorvastatin is the most commonly used of all statins to lower cholesterol. Atorvastatin is extensively metabolized in both gut and liver to produce several active metabolites. The purpose of the present study is to develop a physiologically based pharmacokinetic (PBPK) model for atorvastatin and its two primary metabolites, 2-hydroxy-atorvastatin acid and atorvastatin lactone, using in vitro and in vivo data. The model was used to predict the pharmacokinetic profiles and drug-drug interaction (DDI) effect for atorvastatin and its metabolites in different DDI scenarios. The predictive performance of the model was assessed by comparing predicted results to observed data after coadministration of atorvastatin with different medications such as itraconazole, clarithromycin, cimetidine, rifampin and phenytoin. This population based PBPK model was able to describe the concentration-time profiles of atorvastatin and its two metabolites reasonably well in the absence or presence of those drugs at different dose regimens. The predicted maximum concentration (Cmax), area under the concentration-time curve (AUC) values and between-phase ratios were in good agreement with clinically observed data. The model has also revealed the importance of different metabolic pathways on the disposition of atorvastatin metabolites. This PBPK model can be utilized to assess the safety and efficacy of atorvastatin in the clinic. This study demonstrated the feasibility of applying PBPK approach to predict the DDI potential of drugs undergoing complex metabolism.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data.HPLC of Formula: C33H33FN2O4, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 125995-03-1, in my other articles.

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Tetrahydropyran – Wikipedia,
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