Tag: M.W:500-600

Reference of 125995-03-1, 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.

Expression of OATP2B1 as determinant of drug effects in the microcompartment of the coronary artery

Clinical success of coronary drug-eluting stents (DES) is hampered by simultaneous reduction of smooth muscle cell (HCASMC) and endothelial cell proliferation due to unspecific cytotoxicity of currently used compounds. Previous in vitro data showing SMC-specific inhibition of proliferation suggested that statins may be suitable candidates for DES. It was aim of this study to further investigate statins as DES drug candidates to identify mechanisms contributing to their cell-selectivity. In vitro proliferation assays comparing the influence of various statins on HCASMC and endothelial cells confirmed that atorvastatin exhibits HCASMC-specificity. Due to similar expression levels of the drug target HMG-CoA reductase in both cell types, cellular accumulation of atorvastatin was assessed, revealing enhanced uptake in HCASMC most likely driven by significant expression of OATP2B1, a known uptake transporter for atorvastatin. In accordance with the finding that endogenous OATP2B1 influenced cellular accumulation in HCASMC we used this transporter as a tool to identify teniposide as new DES candidate drug with HCASMC-specific effects. We describe OATP2B1 as a determinant of pharmacokinetics in the coronary artery. Indeed, endogenously expressed OATP2B1 significantly influences the uptake of substrate drugs, thereby governing cell specificity. Screening of candidate drugs for interaction with OATP2B1 may be used to promote SMC-specificity.

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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 Patent£¬once mentioned of 125995-03-1, category: Tetrahydropyrans

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.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

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, COA of Formula: C33H33FN2O4

The metabolism of clopidogrel is catalyzed by human cytochrome P450 3A and is inhibited by atorvastatin

The prodrug clopidogrel (Plavix) is activated by cytochrome P450 (P450) to a metabolite that inhibits ADP-induced platelet aggregation. Clopidogrel is frequently administered to patients in conjunction with the CYP3A4 substrate atorvastatin (Lipitor). Since clinical studies indicate that atorvastatin inhibits the antiplatelet activity of clopidogrel, we investigated whether CYP3A4 metabolized clopidogrel in vitro. Microsomes prepared from dexamethasone-pretreated rats metabolized clopidogrel at a rate of 3.8 nmol min-1 nmol of P450-1, which is 65 and 1270% faster than the rate of metabolism by microsomes from control and beta-napthoflavonetreated rats, respectively. To identify the human P450s responsible for clopidogrel oxidation, genetically engineered microsomes containing a single human P450 isozyme were tested for their ability to oxidize clopidogrel. CYP3A4 and 3A5 metabolized clopidogrel at a significantly higher rate than eight other P450 isozymes, suggesting that CYP3A4 and 3A5 are primarily responsible for in vivo clopidogrel metabolism. Clopidogrel interacts with human CYP3A4 with a spectral dissociation constant (Ks), Km, and Vmax of 12 muM, 14 ¡À muM and 6.7 ¡À 1 nmol min-1 nmol P450-1, respectively. Atorvastatin lactone, the physiologically relevant substrate, inhibits clopidogrel with a KI of 6 muM. When clopidogrel and atorvastatin are present at equimolar concentrations, clopidogrel metabolism is inhibited by greater than 90%. Since CYP3A4 and 3A5 metabolize clopidogrel faster than other human P450 isozymes and are the most abundant P450s in human liver, they are predicted to be predominantly responsible for the activation of clopidogrel in vivo.

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.COA of Formula: C33H33FN2O4, 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 Patent£¬once mentioned of 125995-03-1, Safety of Atorvastatin lactone

NOVEL FORMS OF [R-(R*,R*)]-2-(4-FLUOROPHENYL)-B,B-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPT ANOIC ACID MAGNESIUM

Novel forms of atorvastatin magnesium salt designated Form A, Form B, Form C, Form D, Form E, and Form F, pharmaceutical compositions containing such compounds, methods for their preparation and methods utilizing the compounds for treatment of hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer’s disease are described.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data.Safety of Atorvastatin lactone, 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

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, Safety of Atorvastatin lactone

Supercritical fluid chromatography-tandem mass spectrometry for high throughput bioanalysis of small molecules in drug discovery

Liquid chromatography tandem mass spectrometry (LC?MS/MS) has been a golden standard for high throughput small molecule bioanalysis in drug discovery for decades. Supercritical fluid chromatography (SFC) has caught more attention in recent decade due to its advantages of greener mobile phase, lower backpressure and higher separation power. For the first time, we evaluated supercritical fluid chromatography tandem mass spectrometry (SFC-MS/MS) as a high throughput technique for bioanalysis of small molecule drug candidates and compared it to reversed phase LC?MS/MS. Twenty five compounds with diversified structures were evaluated using combination of 6 achiral columns and 4 different mobile phase compositions. To be able to make direct comparison between SFC and HPLC, same type of mass spectrometer was used as the detector. Extracted biological samples were injected to an SFC-MS/MS system and then re-injected to an LC?MS/MS system. It was found that the success rate of the SFC-MS/MS method development was more than 95% if using certain combinations of achiral column and mobile phase compositions without the time-consuming method scouting process. Sensitivity was established between 0.1 to 5.0 ng/mL for both SFC-MS/MS and LC?MS/MS with better sensitivity on SFC-MS/MS. Data from application studies correlated very well between the data produced by SFC-MS/MS and LC?MS/MS. Approximately 95% samples tested had ?25% difference between SFC-MS/MS and LC?MS/MS data. It was demonstrated that SFC-MS/MS was comparable to golden standard LC?MS/MS and was an alternative choice for routine high throughput bioanalysis of small molecule drugs.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data.Safety of Atorvastatin lactone, 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

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, 125995-03-1.

Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl)ethyl]-2H-pyran-2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing substituents at positions three and four of the pyrrole nucleus

A series of trans-tetrahydro-4-hydroxy-6-[2-(2,3,4,5-substituted-1H-pyrrol-1-yl) ethyl]-2H-pyran-2-ones and their dihydroxy acids were prepared and tested for their ability to inhibit the enzyme HMG-CoA reductase in vitro. Inhibitory potency was found to increase substantially when substituents were introduced into positions three and four of the pyrrole ring. A systematic exploration of structure-activity relationships at these two positions led to the identification of a compound ((+)-33, (+)-(4R)-trans-2-(4-fluorophenyl)-5-(1-methylethyl)-N, 3-diphenyl-1-[(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H- pyrrole-4-carboxamide) with five times the inhibitory potency of the fungal metabolite compactin.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.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, Atorvastatin lactone is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Form A atorvastatin magnesiumA 6.0 g sample of the lactone form of atorvastatin (United States Patent No. 5,273,995) was dissolved in 100 mL of methanol at room temperature. Approximately 11.8 mL of 1 N NaOH (1.05 mol equivalents) was then added to the mixture. The solution was then stirred at 50 0C for approximately 1 hour. A solution of 1.19g MgCI2-SH2O in 5 mL of H2O (0.55 mol equivalents) was then slowly added to the reaction mixture. The mixture was then cooled to room temperature and the resulting precipitate was removed by vacuum filtration through a 0.45-um nylon membrane filter. Approximately 100 mL of H2O was then slowly added to the filtered solution, which caused a white precipitate to form. The resulting suspension was then stirred for approximately 30 minutes. The solid sample was then isolated by vacuum filtration. The filtered solid was then dried under vacuum at 700C for approximately 2 hours to afford 5.8 g of Form A atorvastatin magnesium. Form B atorvastatin magnesiumA 50 mg sample of Form A atorvastatin magnesium (prepared as described above) was slurried in 0.25 mL of ortho-xylene at 45 oC for 28 days using magnetic stirring at 400 rpm. The solid sample was then isolated by centrifuge filtration through a 0.45-mum nylon membrane filter. The filtered solid was then air dried under ambient conditions for approximately 5 hours to afford Form B atorvastatin magnesium., 125995-03-1

125995-03-1 Atorvastatin lactone 6483036, aTetrahydropyrans compound, is more and more widely used in various fields.

Reference£º
Patent; PFIZER PRODUCTS INC.; WO2007/57755; (2007); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.125995-03-1,Atorvastatin lactone,as a common compound, the synthetic route is as follows.

Example 3. Synthesis of Atorva-HA ((3R,5R)-7-[2-(4-Fluoro-phenyl)-5-isopropyl-3- phenyl-4-phenylcarbamoyl pyrrol-l-yl]-3,5-dihydroxy-N-hydroxyheptanamide) [00356] By a procedure similar to Lova-HA, atorvastatin (168 mg, 0.31 mmol, in the lactone form) was treated with MgBr2 (115 mg, 0.62 mmol), hydroxylamine hydrochloride (184 mg, 2.6 mmol), and sodium bicarbonate (209 mg, 2.5 mmol) in anhydrous THF/MeOH (7:3, 1 mL) at ambient temperature for 20 h to give Atorva-HA (91 mg, 51%). The purity was 95% as shown by HPLC analysis on an HC-Cig column (Agilent, 4.6 x 250 mm, 5 muiotaeta), tR = 14.8 min (gradients of 30-100%) aqueous CH3CN in 30 min). C33H36FN305; colorless oil; [alpha]26omicron = -1.3 (EtOAc, c = 1.0); TLC (CH2Cl2/MeOH (9: 1)) Rf= 0.33; IR vmax (neat) 3405, 3301, 3059, 2960, 2926, 1738, 1657, 1595, 1527, 1508, 1436, 1314, 1241, 1223, 1157, 1108, 1078, 1046, 843, 753, 692 cm”1; 1H NMR (DMSO-< 6, 400 MHz) delta 10.31 (1 H, br s), 9.77 (1 H, br s), 8.68 (1 H, br s), 7.50 (2 H, d, J= 7.6 Hz), 7.18-7.24 (6 H, m), 7.07 (4 H, br s), 6.98-7.00 (2 H, m), 4.69 (1 H, br s), 4.60 (1 H, d, J= 4.0 Hz), 3.92-3.95 (1 H, m), 3.72-3.83 (2 H, m), 3.53 (1 H, br s), 3.21-3.25 (1 H, m), 2.01 (2 H, d, J= 6.0 Hz), 1.63 (1 H, br s), 1.53 (1 H, br s), 1.28-1.38 (8 H, m) ppm; 13C NMR (DMS0 , 100 MHz) delta 167.4, 166.1, 162.8, 160.3, 139.4, 135.9, 134.9, 133.4, 129.1 (2 x), 128.7, 128.4 (2 chi), 127.6 (2 chi), 127.3, 125.3, 122.9, 120.6, 119.4 (2 chi), 117.5, 115.4, 115.2, 66.0, 65.6, 43.8, 40.9, 40.7, 25.6, 22.3 (2 chi) ppm; ESI-HRMS (negative mode) calcd. for C33H35FN305: 572.2561, found: m/z 572.2562 [M - H] . 125995-03-1, The synthetic route of 125995-03-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ACADEMIA SINICA; NATIONAL TAIWAN UNIVERSITY; LIANG, Chi-Ming; CHEN, Ching-Chow; CHEN, Jhih-Bin; WEI, Tzu-Tang; LIN, Jung-Hsin; FANG, Jim-Min; CHERN, Ting-Rong; WO2014/15235; (2014); A2;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

125995-03-1, Atorvastatin lactone is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,125995-03-1

An authentic sample of Lactone (530mg) was dissolved in anhydrous DMF (5ML), followed by imidazole (174mg), then TBDMS chloride (371 mg). The mixture was stirred at room temperature. After 6 hours, the reaction was worked up by addition of ET20 (30ML) and water (30ML). The separated organic phase was further washed with water (2 x 20MOI), dried, and concentrated in vacuo to afford silylated lactone as a white powder (470mg, 73%). The silylated lactone (233mg) was dissolved in anhydrous dichloromethane (5ML), then COOLED TO-78C under Nitrogen. DIBAL (0. 31 ml, 1 M in toluene) was added dropwise and the mixture stirred for 10 minutes AT-78C. The mixture was then quenched by addition of 1 ml of 10% aqueous Rochelle’s salt and allowed to warm to room temperature. After addition of further DICHLOROMETHANE (10ML) and water (10MOI), the phases were separated and the organic phase dried and concentrated in vacuo. The residual oil was purified by column chromatography (50% ET20 in hexane). FTIR : 1668 CM~ (amide). Stretch at 1735CM (Lactone) no longer present. The silylated lactol (100mg) was dissolved in anhydrous THF. HF. pyridine was added (0. 1ML) at 0C and allowed to warm to room temperature. The mass was quenched with ether/and sodium bicarbonate solution. The phases separated and the aqueous phase back extracted with ether. The organic phases were combined, dried and evaporated to produce and oil (75mg). M/z 542,524, 506;’H nmr CDC13 1.3 (d, 6H), 1.6- 1.9 (m, 6H), 3.45 (2H), 3.6 (m, 2H), 3.8 (m, 1H), 5.0 (m, 1H), 6.8 (br. s 1H), 7.1 (m, 14H); 3C nmr CDCI3 91.6ppm (Lactol C); FTIR : 1652CM (Amide)

As the paragraph descriping shows that 125995-03-1 is playing an increasingly important role.

Reference£º
Patent; AVECIA LIMITED; WO2005/12246; (2005); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics