Month: April 2021

Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, causing turnover rates to depend strongly on interfacial structure and composition, 31566-31-1, Name is Glyceryl monostearate, SMILES is OCC(O)CO.CCCCCCCCCCCCCCCCCC(O)=O, in an article , author is Ugawa, T, once mentioned of 31566-31-1, Product Details of 31566-31-1.

YM-53601, a novel squalene synthase inhibitor, suppresses lipogenic biosynthesis and lipid secretion in rodents

1 To better understand how it decreases plasma cholesterol and triglyceride levels, we evaluated the effect of (E)-2-[2-fluoro-2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole monohydrochloride (YM-53601) on lipogenic biosynthesis in the liver and lipid secretion from the liver in rats and hamsters. 2 Single administration of YM-53601 in cholestyramine-treated rats inhibited triglyceride and free fatty acid (FFA) biosynthesis at a similar dose range to that at which it inhibited cholesterol biosynthesis. YM-53601 inhibited both triglyceride and FFA biosynthesis in hamsters treated with cholestyramine. 3 YM-53601 by single oral administration decreased the enhanced plasma triglyceride levels in hamsters induced by an injection of protamine sulfate, which inhibits lipoprotein lipase (LPL) and consequently increases plasma very low-density lipoprotein (VLDL) triglyceride levels. YM-53601 also decreased the enhanced plasma triglyceride and cholesterol levels in hamsters treated with Triton WR1339, which also inhibits the degradation of VLDL. Plasma cholesterol was significantly decreased as soon as I h after single administration of YM-53601 in hamsters fed a normal diet. 4 This is the first report that a squalene synthase inhibitor suppresses lipogenic biosynthesis in the liver and cholesterol and triglyceride secretion from the liver in vivo. We therefore suggest that the mechanism by which YM-53601 decreases plasma triglyceride might include these effects. The finding that YM-53601 rapidly decreased plasma cholesterol suggests that this compound may be effective in decreasing plasma cholesterol levels early in the course of treatment of hypercholesterotemia in humans.

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Electric Literature of 871-91-0, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 871-91-0, Name is 7-Octyn-1-ol, SMILES is OCCCCCCC#C, belongs to quinuclidines compound. In a article, author is Gu, Jianhui, introduce new discover of the category.

Convenient new synthesis of umeclidinium bromide

Umeclidinium bromide, a drug used for chronic obstructive pulmonary disease, is synthesized through a new intermediate of phenyl(quinuclidin-4-yl)methanone. This novel method with simple operation flow and cheap reagents, makes it suitable for scale up. The overall four-step process provides umeclidinium bromide in 29% yield and the purity up to 99.83%. The X-ray crystal structure of the drug molecule was first reported.

Electric Literature of 871-91-0, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 871-91-0.

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6753-98-6, Name is (1E,4E,8E)-2,6,6,9-Tetramethylcycloundeca-1,4,8-triene, molecular formula is C15H24, belongs to quinuclidines compound, is a common compound. In a patnet, author is Primozic, Ines, once mentioned the new application about 6753-98-6, Recommanded Product: 6753-98-6.

Binding Modes of Quinuclidinium Esters to Butyrylcholinesterase

The orientations of chiral quinuclidin-3-ol esters and benzoylcholine in the active site of horse butyrylcholinesterase have been investigated by flexible ligand docking. Change of the esters’ acyl moiety as well as the substituent at the quinuclidinium nitrogen atom affected the activity and stereoselectivity of the biotransformations. Analysis of interactions in the active site revealed the most important binding patterns for enantiomers, which define their reactivity. Calculated Gibbs energies of binding obtained by molecular docking simulations were well correlated to the experimentally determined binding affinities of the investigated chiral esters. (doi: 10.5562/cca2060)

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Application of 5405-41-4, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 5405-41-4, Name is Ethyl 3-hydroxybutanoate, SMILES is C(C(OCC)=O)C(C)O, belongs to quinuclidines compound. In a article, author is Dolle, F, introduce new discover of the category.

Highly efficient synthesis of [C-11]Me-QNB, a selective radioligand for the quantification of the cardiac muscarinic receptors using PET

Me-QNB (N-methyl-quinuclidin-3-yl benzilate or N-methyl-quinuclidin-3-yl diphenylhydroxy acetate) is a hydrophilic, non-metabolized and highly specific muscarinic acetylcholinergic antagonist. Using this quaternary ammonium derivative of QNB, labelled with carbon-11, a positron-emitting isotope (half-life : 20.4 minutes), the potential for quantification of myocardial muscarinic receptors in vivo using the high-resolution, sensitive and quantitative imaging technique PET (positron emission tomography) was previously demonstrated in dogs and validated in humans. In this paper, the radiosynthesis of carbon-11-labelled Me-QNB is investigated and oriented towards the preparation of multi milliCuries of radiotracer. Typically, using no-carrier-added [C-11]methyl triflate as the alkylating agent and 0.64 mg (1.89 mu mol) of QNB as precursor for labelling at 100 degreesC for 1 minute lead to a 48.5% +/- 10% (15 runs) decay-corrected radiochemical yield (based on [C-11]methyl triflate). 183 mCi (+/- 39) of [C-11]Me-QNB ([C-11]-1) could be synthesized in only 27 to 28 minutes after EOB and occasionally, up to 340 mCi of [C-11]Me-QNB ([C-11]-1) were obtained, corresponding to a 85% decay-corrected yield. The associated decay-corrected specific radioactivities obtained were 2658 mCi/mu mol (+/- 971) at EOB.

Application of 5405-41-4, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 5405-41-4 is helpful to your research.

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 94-53-1, Name is Benzo[d][1,3]dioxole-5-carboxylic acid, formurla is C8H6O4. In a document, author is BESIDSKY, Y, introducing its new discovery. Recommanded Product: Benzo[d][1,3]dioxole-5-carboxylic acid.

SYNTHESIS AND REACTIVITY OF 6-CARBAMOYL-5-PHENYL-2,3,5,6-TETRAHYDRO-1H-1,4-ETHANOBENZO[F]QUINOLINE – X-RAY MOLECULAR-STRUCTURE OF (4AR-ASTERISK,5S-ASTERISK,6R-ASTERISK,10BR-ASTERISK)-5-PHENYL-2,3,4A,5,6,10B-HEXAHYDRO-1H-1,4-ETHANOBENZO[F]QUINOLIN-6-YL ACETATE

Cyclocondensation of 2-(2-cyano-1,2-diphenylethyl)quinuclidin-3-one 1 in the presence of sulfuric acid gave an intramolecular phenylation instead of lactam formation. The cyclic product was hydrogenated to give 6-carbamoyl-5-phenyl-2,3,4a,5,6,10b-hexahydro-1H-1,4-ethanobenzo- [f]quinoline. On treatment with LiAIH(4) the carbamoyl group was stereospecifically replaced by a hydroxy group. The alcohol was acetylated and the structure was confirmed by X-ray crystallography. The hydroxylation reaction is believed to proceed via a carbonitrile intermediate. In the presence of air the nitrile can be converted to a ketone which is then reduced to the alcohol with an overall retention of configuration.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 94-53-1 help many people in the next few years. Recommanded Product: Benzo[d][1,3]dioxole-5-carboxylic acid.

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Quinuclidine – Wikipedia,
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Synthetic Route of 112-43-6, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 112-43-6, Name is 10-Undecen-1-ol, SMILES is C=CCCCCCCCCCO, belongs to quinuclidines compound. In a article, author is Radl, S, introduce new discover of the category.

Synthesis and antinociceptive activity of some 3-chlorophenyl- and 6-chloropyridin-2-yl derivatives

Derivatives of 2-chloro-6-(4-hydroxy-1-methylpiperidin-4-yl)pyridine (2b) were prepared and tested as analgesics. 2-Chloro-6-lithiopyridine treated with quinuclidin-3-one, 1-methylpyrrolidin-3-one, 2-(dimethylaminomethyl) cyclohexanone, and ethyl 1-methylpiperidin-4-ylcarboxylate provided the corresponding alcohols 5, 6, 13a, and 6-chloro-2-pyridyl 1l-methylpiperidin-4-yl ketone (9). The ketone was reduced with sodium borohydride or treated with methylmagnesium chloride or phenyllithium to provide the corresponding alcohols 11, 12a and 12b, respectively. 1-[4-(6-Chloro-2-pyridyl)1-methyrpiperidin-4-yl]1-methylethanol (4b) was prepared from 2-chloro-6-(1-methyl-1,2,5,6-tetrahydropyridin-4-yl)pyridine (14b) by treatment with butyllithium and acetone followed by reduction of intermediate 15b with sodium cyanoborohydride.

Synthetic Route of 112-43-6, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 112-43-6 is helpful to your research.

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Electric Literature of 147126-62-3, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 147126-62-3, Name is (2R,5R)-(1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl 5-hydroxy-1,3-oxathiolane-2-carboxylate, SMILES is O=C(O[C@H]1[C@@H](CC[C@H](C1)C)C(C)C)[C@@H]2O[C@H](CS2)O, belongs to quinuclidines compound. In a article, author is Shchekotikhin, AE, introduce new discover of the category.

3-aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione for circumvention of anticancer drug resistance

A series of 3-aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3 -f]indole-5,10-dione was synthesized by Mannich reaction or by the transamination of 3-dimethylaminomethyl 4,11-dihydroxy- or 4,11-dimethoxynaphtho[2,3-f]indole-5,10-dione. The potency of novel derivatives was tested on a National Cancer Institute panel of 60 human tumor cell lines as well as in cells with genetically defined determinants of cytotoxic drug resistance, P-glycoprotein (Pgp) expression, and p53 inactivation. Mannich derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione with an additional amino function in their side chain, demonstrated equal cytotoxicity against the parental K562 leukemia cells and their Pgp-positive subline, whereas the latter showed similar to 7-fold resistance to adriamycin, a Pgp transported drug. 3-(1-Piperazinyl)methyl and 3-(quinuclidin-3-yl)aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione killed HCT116 colon carcinoma cells (carrying wild type p53) and their p53-null variant within the similar range of concentrations. We conclude that Mannich modification of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione, especially when cyclic diamine (e.g., piperazine, quinuclidine) is used, confers an important feature to the resulting compounds, namely, the potency for tumor cells otherwise resistant to a variety of anticancer drugs. (c) 2004 Elsevier Ltd. All rights reserved.

Electric Literature of 147126-62-3, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 147126-62-3.

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 116-31-4, Name is trans-Retinal, formurla is C20H28O. In a document, author is Visser, TJ, introducing its new discovery. Safety of trans-Retinal.

Stereoselective synthesis and biodistribution of potent [C-11]-labeled antagonists for positron emission tomography imaging of muscarinic receptors in the airways

Quantitation of muscarinic receptors in the lungs in vivo with positron emission tomography (PET) is of clinical interest. For that purpose we decided to develop [C-11]-labeled ligands with a high affinity (K-D < 0.1 nM). Three quaternary muscarinic antagonists, racemic N-methylpiperidin-4-yl 2-cyclohexy-2-2-hydroxy-2-phenylacetate methiodide 1a (pK(B) = 10.39), its (R)-isomer 1b (pK(B) = 11.08), and (R,R)-quinuclidin-3-yl 2-cyclohexyl-2-hydroxy-2-phenylacetate methiodide 2 (pK(B) = 11.28), were labeled by reacting [C-11]CH3I With their tertiary amine precursors. The enantiomerically pure tertiary amine precursors were prepared by stereoselective synthesis starting from (R)-(-)-mandelic acid. In vitro binding assay of 1b and 2 demonstrated that both ligands bind with very high affinity to the muscarinic receptor subtypes M(1), M(2), and M(3). They are more potent than the muscarinic antagonist (R)-N-methylquinuclidinyl benzilate ((R)-MQNB). Distribution studies with la, 1b, and 2 in control and atropine-treated male Wistar rats demonstrated significant specific binding (90-99% of total issue uptake) in tissues containing cholinoceptors (heart, intestine, lung, pancreas, spleen, stomach, submandibular gland). Because the tissue/plasma concentration ratios of 1b are most favorable, this ligand was used for further evaluation. Analysis of plasma samples showed a very rapid clearance (t(1/2) = 0.3 min) of the radioligand 1b and a relatively slow appearance of a hydrophilic metabolite. At 15 min postinjection of 1b, analysis of heart, lungs, and liver showed that respectively 99%, 88%, and 8% of the tissue radioactivity corresponded with the parent compound. Ligand 1b appears to be an excellent candidate for PET studies of mAChR receptors in heart and lungs. I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 116-31-4 help many people in the next few years. Safety of trans-Retinal.

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Related Products of 301-02-0, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 301-02-0, Name is Oleamide, SMILES is CCCCCCCC/C=CCCCCCCCC(N)=O, belongs to quinuclidines compound. In a article, author is Liu, Yu-Min, introduce new discover of the category.

Stereoselective synthesis of the optical isomers of a new muscarinic receptor antagonist, quinuclidin-3-yl 2-(cyclopent-1-enyl)-2-hydroxy2-phenylacetate

The enantiopure isomers of a new muscarinic receptor antagonist, quinuclidin-3-yl 2-(cyclopent-1-enyl)-2-hydroxy-2-phenylacetate were synthesised by a practical stereoselective synthetic method, using pivaldehyde as steric hindrance agent from the chiral starting material, (S) or (R)-mandelic acid. The isomers were obtained with 72-78% yields in 98-99% e.e.

Related Products of 301-02-0, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 301-02-0.

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Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 141627-42-1, Name is (2-Butyl-5-nitrobenzofuran-3-yl)(4-methoxyphenyl)methanone, SMILES is O=C(C1=C(CCCC)OC2=CC=C([N+]([O-])=O)C=C12)C3=CC=C(OC)C=C3, belongs to quinuclidines compound. In a document, author is Navratil, O, introduce the new discover, SDS of cas: 141627-42-1.

Competitive extraction of some bases by carbollyl-cobaltate anion from water into chloroform

The bis[undecahydro-7,8-dicarbaundecaborato(2-)]cobaltate(1-) (X-) has been used for complementary study of its ionic associates with some cations of organic bases and quaternary salts. For the optimization of present analytical methods, quinuclidin-3-yl hydroxy(diphenyl)acetate, 1-(1-phenylcyclohexyl)piperidine, dibenzo[b,f][1,4]oxazepine and cocaine, were studied by competitive extraction method. X- labelled with Co-60 was used as carrier anion, triphenylmethane and azo dyes as competitive anions, The aqueous phase was 0.1 and 0.01 M HCl, the organic phase was chloroform. A comparison was made with earlier results obtained by extraction spectrophotometry.

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 141627-42-1 is helpful to your research. SDS of cas: 141627-42-1.

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Quinuclidine – Wikipedia,
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