Tag: M.W:500-600

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Patent£¬once mentioned of 125995-03-1, Recommanded Product: Atorvastatin lactone

A process is provided for preparing pharmaceutical grade atorvastatin hemicalcium salt comprising: (a) deesterifying, wherein R is an ester protecting group to (b) extracting R(R*,R*)-3 into an organic solvent or mixture of solvents, (c) adding a base of formula NR1R2R3 wherein R1, R2 and R3 are independently selected from H, substituted or non-substituted C1 to C7 alkyl, C6 to C9 aryl, C8 to C10 aralkyl or aminoalkyl to form atorvastatin base salt, (d) isolating by precipitation of the above atorvastatin base salt and purifying when necessary,

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Recommanded Product: Atorvastatin lactone, you can also check out more blogs about125995-03-1

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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 Article£¬once mentioned of 125995-03-1, SDS of cas: 125995-03-1

Effect of ABCB1 polymorphisms and atorvastatin on sitagliptin pharmacokinetics in healthy volunteers

Objectives: The objectives of this study were to determine if ABCB1 polymorphisms are associated with interindividual variability in sitagliptin pharmacokinetics and if atorvastatin alters the pharmacokinetic disposition of sitagliptin in healthy volunteers. Methods: In this open-label, randomized, two-phase crossover study, healthy volunteers were prospectively stratified according to ABCB1 1236/2677/3435 diplotype (n = 9, CGC/CGC; n = 10, CGC/TTT; n = 10, TTT/TTT). In one phase, participants received a single 100 mg dose of sitagliptin; in the other phase, participants received 40 mg of atorvastatin for 5 days, with a single 100 mg dose of sitagliptin administered on day 5. A 24-h pharmacokinetic study followed each sitagliptin dose, and the study phases were separated by a 14-day washout period. Results: Sitagliptin pharmacokinetic parameters did not differ significantly between ABCB1 CGC/CGC, CGC/TTT, and TTT/TTT diplotype groups during the monotherapy phase. Atorvastatin administration did not significantly affect sitagliptin pharmacokinetics, with geometric mean ratios (90 % confidence intervals) for sitagliptin maximum plasma concentration, plasma concentration-time curve from zero to infinity, renal clearance, and fraction of sitagliptin excreted unchanged in the urine of 0.93 (0.86-1.01), 0.96 (0.91-1.01), 1.02 (0.93-1.12), and 0.98 (0.90-1.06), respectively. Conclusions: ABCB1 CGC/CGC, CGC/TTT, and TTT/TTT diplotypes did not influence sitagliptin pharmacokinetics in healthy volunteers. Furthermore, atorvastatin had no effect on the pharmacokinetics of sitagliptin in the setting of ABCB1 CGC/CGC, CGC/TTT, and TTT/TTT diplotypes.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.SDS of cas: 125995-03-1. 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

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, name: Atorvastatin lactone

The total synthesis of calcium atorvastatin

A practical and convergent asymmetric route to calcium atorvastatin (1) is reported. The synthesis of calcium atorvastatin (1) was performed using the remote 1,5-anti asymmetric induction in the boron-mediated aldol reaction of beta-alkoxy methylketone (4) with pyrrolic aldehyde (3) as a key step. Calcium atorvastatin was obtained from aldehyde (3) after 6 steps, with a 41% overall yield.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.name: Atorvastatin lactone. 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

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, Computed Properties of C33H33FN2O4

The total synthesis of calcium atorvastatin

A practical and convergent asymmetric route to calcium atorvastatin (1) is reported. The synthesis of calcium atorvastatin (1) was performed using the remote 1,5-anti asymmetric induction in the boron-mediated aldol reaction of beta-alkoxy methylketone (4) with pyrrolic aldehyde (3) as a key step. Calcium atorvastatin was obtained from aldehyde (3) after 6 steps, with a 41% overall yield.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Computed Properties of C33H33FN2O4. 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

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., Application In Synthesis of Atorvastatin lactone

Metabolic fate of pitavastatin, a new inhibitor of HMG-CoA reductase: Human UDP-glucuronosyltransferase enzymes involved in lactonization

1. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase little metabolized in hepatic microsomes. Pitavastatin lactone, which can be converted back to the unchanged form, is the major metabolite of pitavastatin in humans. To clarify the mechanism of the lactonization of pitavastatin and the metabolic properties of the lactone, we performed experiments in vitro. 2. On addition of UDP-glucuronic acid, human hepatic microsomes produced pitavastatin lactone and an unknown metabolite (UM-2). UM-2 was converted to its unchanged form by enzymatic hydrolysis and to a lactone form non-enzymatically. Using several human UGT-expressing microsomes, UGT1A3 and UGT2B7 were principally responsible for glucuronidation of pitavastatin leading to lactonization. 3. No marked difference in intrinsic clearance between pitavastatin and its lactone form was detected in human hepatic microsomes. 4. Pitavastatin lactone showed no inhibitory effects on CYP2C9- and CYP3A4-mediated metabolism of model substrates in contrast to other HMG-CoA reductase inhibitors. 5. The mechanism of pitavastatin lactone formation has been clarified, in that glucuronidation by UGT occurs first followed by lactonization via an elimination reaction. It was also found that pitavastatin lactone demonstrates no drug – drug interactions.

Interested yet? Keep reading other articles of 125995-03-1!, Application In Synthesis of Atorvastatin lactone

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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, Safety of Atorvastatin lactone.

ATORVASTATIN STRONTIUM SALT AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

This invention provides atorvastatin strontium salt or its hydrates or polymorphs having improved water solubility, which is useful for the prevention or treatment of hyperlipidemia and hypercholesterolemia, and a pharmaceutical composition comprising same.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Safety of Atorvastatin lactone. 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

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Article£¬once mentioned of 125995-03-1, Safety of Atorvastatin lactone

LC-MS/MS method for quantification of atorvastatin, o-hydroxyatorvastatin, p-hydroxyatorvastatin, and atorvastatin lactone in rat plasma

A simple and sensitive liquid chromatography-tandem mass spectrometry method was developed for the quantification of atorvastatin, ortho-hydroxyatorvastatin, para-hydroxyatorvastatin, and atorvastatin lactone in rat plasma. Solid-phase extraction was used for preparation of samples. Rosuvastatin was chosen as an internal standard. Chromatographic separation was achieved on ZORBAX Eclipse C18 Analytical, 4.6 ¡Á 100 mm (3.5 mum) column with a gradient mobile phase composed of acetonitrile and 0.1% acetic acid, at a flow rate of 400 muL min-1. The column was kept at constant temperature (25 C), and autosampler tray temperature was set at 4 C. The following selected reaction monitoring (SRM) transitions were selected: (m/z, Q1 ? Q3, collision energy) atorvastatin (559.47 ? 440.03, 22 eV), atorvastatin lactone (541.36 ? 448.02, 19 eV), orthohydroxyatorvastatin (575.20 ? 440.18, 20 eV), para-hydroxyatorvastatin (575.54 ? 440.18, 20 eV), and rosuvastatin (482.25 with selected combination of two fragments 257.77, 31 eV, and 299.81, 35 eV) in positive ion mode. The method was validated over a concentration range of 0.5-20 ng mL-1 for ortho-hydroxyatorvastatin and para-hydroxyatorvastatin and 0.1-20 ng mL-1 for atorvastatin and atorvastatin lactone with excellent linearity (r2 = 0.99). This method demonstrated acceptable precision and accuracy at four quality control concentration levels. The detection limits were 0.1 and 0.13 ng mL-1 for orthohydroxyatorvastatin and para-hydroxyatorvastatin, respectively, and 0.05 ng mL-1 for atorvastatin and atorvastatin lactone. All analytes were found to be stable at examined conditions. Validated method was applied for determination of atorvastatin and its metabolites in plasma of experimental animals.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Safety of Atorvastatin lactone, you can also check out more blogs about125995-03-1

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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.Formula: C33H33FN2O4

Systemic Lupus Erythematosus Activity Affects the Sinusoidal Uptake Transporter OATP1B1 Evaluated by the Pharmacokinetics of Atorvastatin

The present study assessed the effect of systemic lupus erythematosus (SLE) activity, a chronic and inflammatory autoimmune disease, on the sinusoidal uptake transporter OATP1B1 using atorvastatin (ATV) as a probe drug. Fifteen healthy subjects, 13 patients with controlled SLE (SLEDAI 0?4), and 12 patients with uncontrolled SLE (SLEDAI from 6 to 15), all women, were investigated. Apparent total clearance of midazolam (MDZ), a marker of CYP3A4 activity, did not vary among the three investigated groups. The controlled and uncontrolled SLE groups showed higher plasma concentrations of MCP-1 and TNF-alpha, while the uncontrolled SLE group also showed higher plasma concentrations of IL-10. The uncontrolled SLE group showed higher area under the curve (AUC) for ATV (60.47 (43.76?83.56) vs. 30.56 (22.69?41.15) ng?hour/mL) and its inactive metabolite ATV-lactone (98.74 (74.31?131.20) vs. 49.21 (34.89?69.42) ng?hour/mL), and lower apparent total clearance (330.7 (239.30?457.00) vs. 654.5 (486.00?881.4) L/hour) and apparent volume of distribution (2,609 (1,607?4,234) vs. 7,159 (4,904?10,450) L), when compared to the healthy subjects group (geometric mean and 95% confidence interval). The pharmacokinetics of ATV and its metabolites did not differ between the healthy subject group and the patients with controlled SLE group. In conclusion, uncontrolled SLE increased the systemic exposure to both ATV and ATV-lactone, inferring inhibition of OATP1B1 activity, once in vivo CYP3A4 activity assessed by oral clearance of MDZ was unaltered. The inflammatory state, not the disease itself, was responsible for the changes described in the uncontrolled SLE group as a consequence of inhibition of OATP1B1, because systemic exposure to ATV and its metabolites were not altered in patients with controlled SLE.

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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 Article£¬once mentioned of 125995-03-1, COA of Formula: C33H33FN2O4

A comparison of the effects of 3-hydroxy-3-methylglutaryl-coenzyme a (HMG-CoA) reductase inhibitors on the CYP3A4-dependent oxidation of mexazolam in vitro

HMG-CoA reductase inhibitors can be divided into two groups: those administered as the prodrug, i.e., the lactone form (e.g., simvastatin and lovastatin), and those administered in the active form, i.e., the acid form (e.g., pravastatin, fluvastatin, atorvastatin, and cerivastatin). In this study, the influence of the lactone and acid forms of various HMG-CoA reductase inhibitors on metabolism by CYP3A4, a major cytochrome P450 isoform in human liver, was investigated by determining the in vitro inhibition constant (Ki value) using an antianxiety agent, mexazolam, as a probe substrate. In human liver microsomes, all the lactone forms tested inhibited the oxidative metabolism of mexazolam more strongly than did the acid forms, which have lower partition coefficient (logD7.0) values. In addition, the degree of inhibition of mexazolam metabolism tended to increase with an increasing logD7.0 value of the HMG-CoA reductase inhibitors among the lactone and acid forms. In particular, pravastatin (acid form), which has the lowest logD7.0 value, failed to inhibit CYP3A4 activity. Taking account of the lipophilicity of the inhibitors, in conjunction with the CYP3A4-inhibitory activity, could be very useful in predicting drug interactions between substrates of CYP3A4 and HMG-CoA reductase inhibitors.

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£º
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 Review£¬once mentioned of 125995-03-1, Product Details of 125995-03-1

Critical review of statins: A bio-analytical perspective for?therapeutic?drug monitoring

Statins are amongst the most prescribed agents worldwide for treating hypercholesterolaemia. This review summarizes bio-analytical techniques for monitoring of presently available seven statins- Atorvastatin, Rosuvastatin, Pitavastatin, Simvastatin, Lovastatin, Pravastatin and Fluvastatin with a special focus on sample preparation strategies and chromatographic analysis. Applications include determination of statins in various biological fluids like plasma, serum and urine. Apart from conventional extraction procedures of Protein precipitation, Liquid?liquid extraction and Solid-phase extraction, various novel extraction techniques like Micro-extraction by packed sorbent, Dispersive liquid?liquid micro-extraction, Salting-out assisted liquid?liquid extraction etc. are also used for sample clean-up. Extracted samples are usually separated by reverse-phase HPLC and quantitated either by UV or MS/MS detection. The importance and use of chromatographic techniques to separate drug-related biotransformation products are also discussed herein. Most bio-analytical techniques allow quantitation of statins in ng/ml range making them suitable for therapeutic monitoring of statins in routine.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data.Product Details of 125995-03-1, 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£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics