Tag: M.W:500-600

Computed Properties of C33H33FN2O4. In homogeneous catalysis, catalysts are in the same phase as the reactants. Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. Introducing a new discovery about 125995-03-1, Name is Atorvastatin lactone

Background: Statins have anticancer effects on prostate cancer both in vitro and in vivo. It is unclear whether this is due to systemic cholesterol-lowering or direct local growth inhibition in the prostate. It is also unclear whether statins can access the prostate; lipophilic statins could, in theory, pass lipid-enriched cell membranes by passive diffusion. However, statin concentrations in the human prostate have not been measured before. Methods: The study population was based on a randomized clinical trial where 158 men with prostate cancer were randomized to use 80 mg atorvastatin (ATV) or placebo daily for a median of 27 days before radical prostatectomy. ATV and atorvastatin lactone (ATV-Lactone) concentrations in the plasma and in the prostate were measured with mass spectrometry in men randomized to the ATV arm. Linear trends between intraprostatic concentration and plasma concentration, body mass index, age, and duration of intervention were examined. The relative tissue concentrations of ATV and ATV-Lactone were calculated in prostatic tissue and plasma to evaluate drug homeostasis. Subgroup analyses were stratified by tumor and population characteristics. Results: The analysis involved a total of 55 men. When limited to men whose tissue concentrations of ATV was measurable (n = 28, 50%), median ATV concentration was 212% higher in the tissue (median concentration 17.6 ng/g) compared to the plasma (median concentration 3.6 ng/mL). Also, ATV-L concentration was 590% higher in the tissue as compared to the plasma concentration. No statistically significant linear trends between the plasma and tissue concentrations were observed. When comparing the relative concentration of atorvastatin lactone over ATV, the concentrations were in balance in the plasma, In the prostate, however, the relative concentration of atorvastatin lactone was 57% lower compared to ATV (P =.009 for the difference between prostate tissue and plasma). No effect modification by tumor or population characteristics was observed. Conclusions: Measurable ATV concentrations in the prostate support ATV’s ability to access the prostate from the circulation. ATV may accumulate in the prostate as intraprostatic concentrations are elevated compared to the plasma concentration.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data.Computed Properties of 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,
Tetrahydropyran – an overview | ScienceDirect Topics

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 Article，once mentioned of 125995-03-1, Reference of 125995-03-1

We synthesized 11 kinds of prodrug with an esterified carboxylic acid moiety of atorvastatin in moderate to high yields. We discovered that they underwent metabolic activation specifically by the human carboxylesterase 1 (CES1) isozyme. The results suggested that these ester compounds of atorvastatin have the potential to act as prodrugs in vivo.

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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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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, C33H33FN2O4. A document type is Article, introducing its new discovery., name: Atorvastatin lactone

Purpose. With the growing clinical usage of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (statins), the number of reports concerning serious drug-drug interaction has been increasing. Because recent studies have shown that conversion between acid and lactone forms occurs in the body, drug-drug interaction should be considered on both acid and lactone forms. Thus, we investigated the inhibitory effects of acid and lactone forms of eight statins, including one recently withdrawn, cerivastatin, and two recently developed, pitavastatin and rosuvastatin, on cytochrome P450 (CYP) 2C8, CYP2C9, and CYP3A4/5 metabolic activities and multidrug resistance protein 1 (MDR1) transporting activity. Methods. The inhibitory effects of statins on CYP metabolic activities and MDR1 transporting activity were investigated using human liver microsomes and MDR1-overexpressing LLC-GA5-COL150 cells, respectively. Results. The acid forms had minimal inhibitory effects on all CYP activities tested, except for fluvastatin on CYP2C9-mediated tolbutamide 4-hydroxylation (IC50 = 1.7 muM) and simvastatin on CYP3A4/5-mediated paclitaxel 3-hydroxylation (12.0 muM). Lactone forms showed no or minimal inhibitory effects on CYP2C8, CYP2C9, and CYP2C19 activities, except for rosuvastatin on the CYP2C9 activity (20.5 muM), whereas they showed stronger inhibitory effects on the CYP3A4/5 activity with the rank order of atorvastatin (5.6 muM), cerivastatin (8.1 muM), fluvastatin (14.9 muM), simvastatin (15.2 muM), rosuvastatin (20.7 muM), and lovastatin (24.1 muM). Pitavastatin and pravastatin had little inhibitory effect, and a similar order was found also for testosterone 6beta-hydroxylation. MDR1-mediated transport of [3H]digoxin was inhibited only by lactone forms, and the rank order correlated with that of inhibitory effects on both CYP3A4/5 activities. Inhibitory effects on MDR1 activity, and on both CYP3A4/5 activities, could be explained by the lipophilicity; however, a significant correlation was found between the lipophilicity and inhibitory effects on CYP2C8-mediated paclitaxel 6alpha-hydroxylation. Conclusions. We showed the difference between the acid and lactone forms in terms of drug interaction. The lipophilicity could be one of the important factors for inhibitory effects. In the case of statins, it is important to examine the effects of both forms to understand the events found in clinical settings, including the pleiotropic effects.

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Tetrahydropyran – Wikipedia,
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125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4, belongs to tetrahydropyrans compound, is a common compound. In a patnet, once mentioned the new application about 125995-03-1, category: Tetrahydropyrans

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.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.category: Tetrahydropyrans. In my other articles, you can also check out more blogs about 125995-03-1

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Chapter，once mentioned of 125995-03-1, COA of Formula: C33H33FN2O4

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.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data.COA 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.

Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4, belongs to tetrahydropyrans compound, is a common compound. In a patnet, once mentioned the new application about 125995-03-1, COA of Formula: C33H33FN2O4

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.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.COA of Formula: C33H33FN2O4. In my other articles, you can also check out more blogs about 125995-03-1

Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Patent，once mentioned of 125995-03-1, Safety of Atorvastatin lactone

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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Tetrahydropyran – Wikipedia,
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Reference of 125995-03-1. Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 125995-03-1, Name is Atorvastatin lactone

Systems Pharmacology Dissection of Cholesterol Regulation Reveals Determinants of Large Pharmacodynamic Variability between Cell Lines

In individuals, heterogeneous drug-response phenotypes result from a complex interplay of dose, drug specificity, genetic background, and environmental factors, thus challenging our understanding of the underlying processes and optimal use of drugs in the clinical setting. Here, we use mass-spectrometry-based quantification of molecular response phenotypes and logic modeling to explain drug-response differences in a panel of cell lines. We apply this approach to cellular cholesterol regulation, a biological process with high clinical relevance. From the quantified molecular phenotypes elicited by various targeted pharmacologic or genetic treatments, we generated cell-line-specific models that quantified the processes beneath the idiotypic intracellular drug responses. The models revealed that, in addition to drug uptake and metabolism, further cellular processes displayed significant pharmacodynamic response variability between the cell lines, resulting in cell-line-specific drug-response phenotypes. This study demonstrates the importance of integrating different types of quantitative systems-level molecular measurements with modeling to understand the effect of pharmacological perturbations on complex biological processes. Blattmann et al. combine proteomic and metabolomic profiling with mechanistic modeling to characterize the complex processes underlying the heterogeneous drug response in cellular cholesterol regulation across a panel of different human cell lines.

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Tetrahydropyran – Wikipedia,
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Electric Literature of 125995-03-1, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Patent，once mentioned of 125995-03-1

Process for the preparation of amorphous atorvastatin calcium

A process for the preparation of amorphous atorvastatin calcium and hydrates thereof, which comprises: (a) hydrolysis of the precursor lactone using sodium hydroxide to form atorvastatin sodium salt solution; (b) addition of the atorvastatin sodium salt solution to a calcium chloride or calcium acetate solution in the absence or presence of seeds of amorphous atorvastatin calcium; and (c) isolation of the resultant amorphous atorvastatin calcium salt by filtration and drying.

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 125995-03-1 is helpful to your research., Electric Literature of 125995-03-1

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Tetrahydropyran – Wikipedia,
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