A new application about 5291-32-7

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An article , which mentions 5291-32-7, molecular formula is C10H17NO3. The compound – APR-246 played an important role in people’s production and life., Formula: C10H17NO3

Piperlongumine and p53-reactivator APR-246 selectively induce cell death in HNSCC by targeting GSTP1

TP53 mutations frequently occur in head and neck squamous cell carcinoma (HNSCC) patients without human papillomavirus infection. The recurrence rate for these patients is distinctly high. It has been actively explored to identify agents that target TP53 mutations and restore wild-type (WT) TP53 activities in HNSCC. PRIMA-1 (p53-reactivation and induction of massive apoptosis-1) and its methylated analogue PRIMA-1Met (also called APR-246) were found to be able to reestablish the DNA-binding activity of p53 mutants and reinstate the functions of WT p53. Herein we report that piperlongumine (PL), an alkaloid isolated from Piper longum L., synergizes with APR-246 to selectively induce apoptosis and autophagic cell death in HNSCC cells, whereas primary and immortalized mouse embryonic fibroblasts and spontaneously immortalized non-tumorigenic human skin keratinocytes (HaCat) are spared from the damage by the co-treatment. Interestingly, PL-sensitized HNSCC cells to APR-246 are TP53 mutation-independent. Instead, we demonstrated that glutathione S-transferase pi 1 (GSTP1), a GST family member that catalyzes the conjugation of GSH with electrophilic compounds to fulfill its detoxification function, is highly expressed in HNSCC tissues. Administration of PL and APR-246 significantly suppresses GSTP1 activity, resulting in the accumulation of ROS, depletion of GSH, elevation of GSSG, and DNA damage. Ectopic expression of GSTP1 or pre-treatment with antioxidant N-acetyl-l-cysteine (NAC) abrogates the ROS elevation and decreases DNA damage, apoptosis, and autophagic cell death prompted by PL/APR-246. In addition, administration of PL and APR-246 impedes UMSCC10A xenograft tumor growth in SCID mice. Taken together, our data suggest that HNSCC cells are selectively sensitive to the combination of PL and APR-246 due to a remarkably synergistic effect of the co-treatment in the induction of ROS by suppression of GSTP1.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H170N | ChemSpider

Discovery of Quinuclidin-3-yl acetate

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827-61-2, Name is Quinuclidin-3-yl acetate, belongs to quinuclidine compound, is a common compound. HPLC of Formula: C9H15NO2In an article, once mentioned the new application about 827-61-2.

Boronic acid adducts of rhenium dioxime and technetium-99m dioxime complexes containing a biochemically active group

Boronic acid adducts of technetium-99m and radioactive rhenium dioxime complexes, each of which include biochemically active groups, are useful as diagnostic and therapeutic agents, respectively.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H41N | ChemSpider

Awesome and Easy Science Experiments about 827-61-2

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Application of 827-61-2, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.827-61-2,Quinuclidin-3-yl acetate. In a Patent£¬once mentioned of 827-61-2

COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF EYE DISORDERS AND SKIN DISEASES

Disclosed is a compound of formula I or a pharmaceutically acceptable hydrate, solvate, crystal, co-crystal, enantiomer, stereoisomer, polymorph or prodrug thereof, which is useful for treatment of eye disorders, skin diseases and/or complications associated therewith. Also disclosed is a pharmaceutical composition comprising as an active ingredient at least one compound of formula I and a pharmaceutically acceptable excipient. Also disclosed is a method of treating an eye disorder, skin disease and/or a complication thereof in a subject in need thereof by administering at least one compound of formula I or a pharmaceutically acceptable hydrate, solvate, crystal, co-crystal, enantiomer, stereoisomer, polymorph or prodrug thereof.

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H40N | ChemSpider

Discovery of 827-61-2

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Drugs, leads, and drug-likeness: an analysis of some recently launched drugs.

An analysis of the origins of recently launched drugs reveals that most were derived by modification of known drug structures or from lead structures obtained from the scientific literature. High-throughput screening did not have a significant impact on the derivation of these drugs. The drug structures are very closely related to their leads.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H79N | ChemSpider

More research is needed about Quinuclidin-4-ylmethanamine

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 67496-78-0, and how the biochemistry of the body works.Product Details of 67496-78-0

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 67496-78-0, Name is Quinuclidin-4-ylmethanamine,introducing its new discovery., Product Details of 67496-78-0

BENZIMIDAZOLE COMPOUNDS

This invention relates to compounds useful in treating 5-HT. sub.4 and/or 5-HT 3 mediated conditions of the formula STR1 or a pharmaceutically acceptable salt thereof wherein R 1 and R 2 are independently selected from the group consisting of hydrogen, alkoxy, halogen, amino, monoalkylamino, dialkylamino, acylamino and alkylsulfonylamino; R 3 is selected from the group consisting of H, alkyl and cycloalkyl; X is NH or O; and Z is selected from the group consisting of STR2 pharmaceutical compositions including the compounds and a method for treating serotonin mediated conditions with the compositions which act as 5-HT 4 agonists or antagonists and/or 5-HT. sub.3 antagonists.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 67496-78-0, and how the biochemistry of the body works.Product Details of 67496-78-0

Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H14N | ChemSpider

Extracurricular laboratory:new discovery of (R)-3-Aminoquinuclidine dihydrochloride

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, category: quinuclidine, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about category: quinuclidine

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. category: quinuclidine, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 123536-14-1, name is (R)-3-Aminoquinuclidine dihydrochloride. In an article£¬Which mentioned a new discovery about 123536-14-1

QUINUCLIDINES SUBSTITUTED BENTODIOXINE CARBOXAMIDES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

The invention provides the malate salt of compounds of Formula I, wherein X is malate salt, including D- or L-; wherein A is (a), wherein B is (b) or pharmaceutical composition, racemic mixture, or pure enantiomer thereof. The compounds of Formula I are useful to treat diseases or conditions in which alpha7 is known to be involved.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H130N | ChemSpider

Top Picks: new discover of 827-61-2

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Visible-Light-Mediated Metal-Free Difunctionalization of Alkenes with CO2 and Silanes or C(sp3)?H Alkanes

Catalytic alkene difunctionalization via Si?H and C?H activations represents an ideal atom- and step-economic pathway for quick assembly of molecular complexity. We herein developed a visible-light-promoted metal-free difunctionalization of alkenes using abundant CO2 and readily available Si?H and C(sp3)?H bonds as feedstocks. Through the merger of photoredox and hydrogen-atom-transfer catalysis, a variety of value-added compounds, such as beta-silacarboxylic acids and acids bearing a gamma-heteroatom (e.g., N, O, S) could be directly accessed from simple alkenes in a redox-neutral fashion.

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H63N | ChemSpider

New explortion of (R)-3-Aminoquinuclidine dihydrochloride

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 123536-14-1, and how the biochemistry of the body works.name: (R)-3-Aminoquinuclidine dihydrochloride

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride. In a document type is Article, introducing its new discovery., Product Details of 123536-14-1

Synthesis, crystal structures, second harmonic generation response and temperature phase transitions of two noncentrosymmetric Cu(II)-hybrid halides compounds: [(R)-C7H16N2][CuX4] (X = Cl or Br)

(R)-(+)-3-aminoquinuclidine was used in the synthesis of [(R)-C7H16N2][CuCl4] (1) and [(R)-C7H16N2][CuBr4] (2), which both contain similar [CuX4]2- anions (X = Cl or Br). The structures of the two compounds were determined using single-crystal X-ray diffraction. The use of enantiomerically pure sources of (R)-C7H14N2 forces crystallographic noncentrosymmetry. These materials crystallize in the chiral space group P212121 (No. 19), which exhibits the enantiomorphic crystal class 222 (D2). In the molecular arrangement, the [CuX4]2- anions are linked to the organic cations through N?H ? X and C?H ? X hydrogen bonds to form cation-anion-cation molecular units, which are held together by means of offset face-to-face interactions giving a three-dimensional network. Thermal stability of the crystals was ascertained by TG measurement. Compounds (1) and (2) display several phases transition with higher transition temperature at T = 100 C. The Kurtz and Perry powder method using Nd:YAG laser shows that their second harmonic generation (SHG) efficiencies are about 0.81 and 0.82 times as large as that of KH2PO4 (KDP), respectively. Such a chiral hybrid metal halides skeleton could provide a new platform for future engineering in the areas including information storage, light modulators and optoelectronic functionalities.

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H145N | ChemSpider

Properties and Exciting Facts About (R)-3-Aminoquinuclidine dihydrochloride

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 123536-14-1, and how the biochemistry of the body works.Application of 123536-14-1

Application of 123536-14-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a Article£¬once mentioned of 123536-14-1

Discovery of fused heterocyclic carboxamide derivatives as novel alpha7-nAChR agonists: Synthesis, preliminary SAR and biological evaluation

The alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) has emerged as a promising therapeutic target for schizophrenia. In our previous work, a novel series of alpha7-nAChR agonists bearing scaffold of indolizine were discovered. To explore the effect of aromaticity on the activity and find more active agents, herein, fused heterocyclic carboxamide derivatives were designed and synthesized in this study. Based on the evaluation by two-electrode voltage clamp in Xenopus oocytes, 27 of the synthesized compounds showed obvious agonism of alpha7 nAChR. Particularly, compounds 10a and 10e showed significantly higher Emax than EVP-6124. The result illustrated the importance of aromaticity to the activity of agonism. Compound 10a, which showed EC50 of 1.88 muM and Emax of 72.4%, was further characterized comprehensively, including co-application with type II positive allosteric modulator PNU-120596, selectivity with other closely related ligand-gated ion channel, etc. The results showed that 10a showed moderate selectivity over other subtypes such as alpha4beta2 and alpha3beta4 nAChR. 10a evoked alpha7-like currents that were inhibited by MLA and enhanced in the presence of the alpha7 PAM PNU-120596. The analysis of binding mode and understanding of structure-activity relationship provided insights to develop more potent novel alpha7-nAChR agonists.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 123536-14-1, and how the biochemistry of the body works.Application of 123536-14-1

Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H158N | ChemSpider

New explortion of Quinuclidin-3-yl acetate

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Pharmacological strategies for presbyopia correction

Purpose: To summarize the pharmacological strategies that are being explored for presbyopia correction. Methods: The review concentrates on pharmacologically induced pupillary miosis to increase depth-of-focus and lens softening or other measures to restore active accommodation. Results: Several studies suggest that near vision improves and distance vision is unaffected for many hours after either monocular or binocular instillation of any one of several drug combinations that cause miosis. Unfortunately, in most studies, measurements were limited to photopic visual acuity for near and distance vision, whereas it is anticipated that pupil constriction may have adverse effects on mesopic and scotopic vision. It is not clear whether improved near vision was due entirely to increased depth-of-focus, or whether, for example, a drug-induced myopic shift in refraction was also involved. Currently, no study has provided direct evidence for drug-induced restoration/enhancement of true accommodation involving an ocular power change. Conclusions: Although it is possible that, in the future, pharmacological drops may offer a safe and reliable solution for presbyopia correction, more evidence of their effectiveness and limitations is required.

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H74N | ChemSpider