Tag: 0-100

Shi, Jinfeng; Ren, Yali; Ma, Jiaqi; Luo, Xi; Li, Jiaxin; Wu, Yihan; Gu, Huan; Fu, Chaomei; Cao, Zhixing; Zhang, Jinming published their research in Journal of Nanobiotechnology in 2021. The article was titled 《Novel CD44-targeting and pH/redox-dual-stimuli-responsive core-shell nanoparticles loading triptolide combats breast cancer growth and lung metastasis》.Synthetic Route of C4H11NO The article contains the following contents:

The toxicity and inefficient delivery of triptolide (TPL) in tumor therapy have greatly limited the clin. application. Thus, we fabricated a CD44-targeting and tumor microenvironment pH/redox-sensitive nanosystem composed of hyaluronic acid-vitamin E succinate and poly (β-amino esters) (PBAEss) polymers to enhance the TPL-mediated suppression of breast cancer proliferation and lung metastasis. The generated TPL nanoparticles (NPs) had high drug loading efficiency (94.93% ± 2.1%) and a desirable average size (191 nm). Mediated by the PBAEss core, TPL/NPs displayed a pH/redox-dual-stimuli-responsive drug release profile in vitro. Based on the hyaluronic acid coating, TPL/NPs exhibited selective tumor cellular uptake and high tumor tissue accumulation capacity by targeting CD44. Consequently, TPL/NPs induced higher suppression of cell proliferation, blockage of proapoptotic and cell cycle activities, and strong inhibition of cell migration and invasion than that induced by free TPL in MCF-7 and MDA-MB-231 cells. Importantly, TPL/NPs also showed higher efficacy in shrinking tumor size and blocking lung metastasis with decreased systemic toxicity in a 4T1 breast cancer mouse model at an equivalent or lower TPL dosage compared with that of free TPL. Histol. immunofluorescence and immunohistochem. analyses in tumor and lung tissue revealed that TPL/NPs induced a high level of apoptosis and suppressed expression of matrix metalloproteinases, which contributed to inhibiting tumor growth and pulmonary metastasis. Collectively, our results demonstrate that TPL/NPs, which combine tumor active targeting and pH/redox-responsive drug release with proapoptotic and antimobility effects, represent a promising candidate in halting breast cancer progression and metastasis while minimizing systemic toxicity. In the experimental materials used by the author, we found 4-Aminobutan-1-ol(cas: 13325-10-5Synthetic Route of C4H11NO)

4-Aminobutan-1-ol(cas: 13325-10-5) is used in the synthesis of NSAIDs with anti-inflammatory properties. Also used in the synthesis of polyamine transport ligands with specificity against human cancers allowing easy access to specific cancer cells.Synthetic Route of C4H11NO

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《Nanoparticle depots for controlled and sustained gene delivery》 was written by Li, Zhongyu; Ho, William; Bai, Xin; Li, Fengqiao; Chen, Yen-jui; Zhang, Xue-Qing; Xu, Xiaoyang. Safety of 4-Aminobutan-1-ol And the article was included in Journal of Controlled Release in 2020. The article conveys some information:

Gene therapy is one of the most promising medical fields which holds the potential to rapidly advance the treatment of difficult ailments such as cancer as well as inherited genetic diseases. However, clin. translation is limited by several drug delivery hurdles including renal clearance, phagocytosis, enzymic degradation, protein absorption, as well as cellular internalization barriers. Addnl., successful treatments require sustained release of drug payloads to maintain the effective therapeutic level. As such, controlled and sustained release is a significant concern as the localization and kinetics of nucleic acid therapeutics can significantly influence the therapeutic efficacy. This is an unmet need which calls for the development of controlled-release nanoparticle (NP) technologies to further improve the gene therapy efficacy by prolonging the release of nucleic acid drug payload for sustained, long-term gene expression or silencing. Herein, we present a polymeric NP system with sustained gene delivery properties, which can be synthesized using biodegradable and biocompatible polymers via self-assembly. The NP delivery system is composed of a polymeric NP which acts as a drug depot encapsulating cationic polymer/nucleic acid complexes, facilitating the enhanced retention and prolonged release of the gene payload. The NPs showed excellent cellular biocompatibility and gene delivery efficacy using the green fluorescent protein (GFP) encoded DNA plasmid (pGFP) as a reporter gene. Sustained release of the pGFP payload was shown over a period of 8 days. The physicochem. properties such as morphol., particle size, zeta potential, pGFP encapsulation efficiency and biol. properties such as pGFP release profile, in vitro cytotoxicity and transfection efficacy in Hek 293 cells were characterized and evaluated. Importantly, the NP-mediated sustained release of pGFP generates enhanced GFP expression over time. We expect this NP-mediated gene delivery system to provide safe and sustained release of various nucleic acid-based therapeutics with applications in both fundamental biol. studies and clin. translations. In addition to this study using 4-Aminobutan-1-ol, there are many other studies that have used 4-Aminobutan-1-ol(cas: 13325-10-5Safety of 4-Aminobutan-1-ol) was used in this study.

4-Aminobutan-1-ol(cas: 13325-10-5) is used in the synthesis of NSAIDs with anti-inflammatory properties. Also used in the synthesis of polyamine transport ligands with specificity against human cancers allowing easy access to specific cancer cells.Safety of 4-Aminobutan-1-ol

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Lewin, Anita H.; Brieaddy, Larry; Deschamps, Jeffrey R.; Imler, Gregory H.; Mascarella, S. Wayne; Reddy, P. Anantha; Carroll, F. Ivy published an article on January 16 ,2019. The article was titled 《Synthesis and Characterization of the Selective, Reversible PKCβ Inhibitor (9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione, Ruboxistaurin (LY333531)》, and you may find the article in ACS Chemical Neuroscience.Reference of (R)-Oxiran-2-ylmethanol The information in the text is summarized as follows:

The demonstrated role of PKCβ in mediating amphetamine-stimulated dopamine efflux, which regulates amphetamine-induced dopamine transporter trafficking and activity, has promoted the research use of the selective, reversible PKCβ inhibitor (9S)-9-[(dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione, ruboxistaurin. Despite the interest in development of ruboxistaurin as the mesylate monohydrate (Arxxant) for the treatment of diabetic retinopathy, macular edema, and nephropathy, several crucial details in physicochem. characterization were erroneous or missing. This report describes the synthesis and full characterization of ruboxistaurin free base (as a monohydrate), including X-ray crystallog. to confirm the absolute configuration, and of the mesylate salt, isolated as a hydrate containing 1.5 mol of water per mol.(R)-Oxiran-2-ylmethanol(cas: 57044-25-4Reference of (R)-Oxiran-2-ylmethanol) was used in this study.

(R)-Oxiran-2-ylmethanol(cas: 57044-25-4) is a chiral building block used to construct an epoxyvinyl iodide intermediate in a synthesis of a furanocembrane, a marine natural product.Reference of (R)-Oxiran-2-ylmethanol

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Recommanded Product: (R)-Oxiran-2-ylmethanolOn October 15, 2020 ,《Determining the relative reactivity of sulfate, bisulfate, and organosulfates with epoxides on secondary organic aerosol》 was published in ACS Earth and Space Chemistry. The article was written by Aoki, Erika; Sarrimanolis, Jon N.; Lyon, Sophie A.; Elrod, Matthew J.. The article contains the following contents:

Extensive laboratory and field studies have identified nucleophilic addition reactions of isoprene epoxydiols (IEPOX) as key pathways for the formation of isoprene-derived secondary organic aerosol (SOA). Organosulfates are important reaction products of these processes, but it is unclear whether sulfate and/or bisulfate nucleophiles are responsible for their formation and whether the organosulfates themselves can serve as nucleophiles in oligomer-forming reactions. The relative reactivities (nucleophilic strengths relative to water) of sulfate, bisulfate, and Me sulfate anion were measured through a series of model epoxide-nucleophile experiments using NMR (NMR) spectroscopy. These experiments also helped establish a rigorous understanding of the effects of differing carbon substitution and functional groups of epoxides on the modulation of the effective nucleophilicites of sulfate, bisulfate, and Me sulfate anions. It was determined that the nucleophilicites of bisulfate and Me sulfate anions were about 100 and 50 times, resp., weaker than sulfate toward most of the epoxides studied, which was rationalized by computational estimates of their thermodn. basicities. Therefore, for most SOA acidity situations, sulfate-epoxide reactions are expected to be the main source of organosulfate aerosol constituents. Because sulfate-epoxide reactions stoichiometrically consume acid, these reactions also have the capability of raising the pH of SOA, thus slowing down all acid-catalyzed chem. processes. No evidence for the reaction of the Me sulfate anion was observed with the abundant atmospherically relevant epoxide, trans-β-IEPOX, thus suggesting that oligomerization reactions via epoxide-organosulfate reactions may not be able to compete with stronger (such as sulfate) or more abundant (such as water) nucleophiles on actual SOA.(R)-Oxiran-2-ylmethanol(cas: 57044-25-4Recommanded Product: (R)-Oxiran-2-ylmethanol) was used in this study.

(R)-Oxiran-2-ylmethanol(cas: 57044-25-4) is a chiral building block used to construct an epoxyvinyl iodide intermediate in a synthesis of a furanocembrane, a marine natural product.Recommanded Product: (R)-Oxiran-2-ylmethanol

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《Selective synthesis of alkyl amines and N-vinylazoles from vinyl sulfonium salts with N-nucleophiles》 was written by Zou, Liang-Hua; Liu, Biao; Wang, Cheng; Shao, Zeyu; Zhou, Junqi; Shao, Andong; Wen, Jian. Recommanded Product: Oxetan-3-olThis research focused onvinyltetrahydrothiophenium salt amine coupling; sulfanylalkylamine preparation green chem; alkenyl amine preparation green chem. The article conveys some information:

An efficient and green method for the synthesis of various alkyl amines via the C(sp3)-S bond cleavage of vinylsulfonium salts was developed. The reaction proceeded under air atm. with a broad scope of N-nucleophiles ranging from primary and secondary alkyl and aryl amines to various N-containing heterocycles. Moreover, in the presence of a base, the reaction of vinylsulfonium salts with N-containing heterocycles at room temperature can also afford N-vinylazoles with moderate to good yields. Finally, the practicality of this protocol was demonstrated by one-pot reaction, scale-up reaction and product derivatization. In addition to this study using Oxetan-3-ol, there are many other studies that have used Oxetan-3-ol(cas: 7748-36-9Recommanded Product: Oxetan-3-ol) was used in this study.

Oxetan-3-ol(cas: 7748-36-9) is used as a reagent in the synthesis of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. It is also used as a reagent in the synthesis of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors.Recommanded Product: Oxetan-3-ol

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Computed Properties of C3H6O2In 2021 ,《Synthesis of Terminal N-Vinylazoles from Aromatic Aldehydes, DMSO, and Azoles Based DMSO as Terminal Carbon Synthon》 was published in Advanced Synthesis & Catalysis. The article was written by Nie, Zhiwen; Lv, Huifang; Li, Hui; Su, Miaodong; Yang, Tonglin; Luo, Weiping; Liu, Qiang; Guo, Cancheng. The article contains the following contents:

A protocol for the synthesis of terminal N-vinylazoles such as H2C=CR1R [R = indol-1-yl, pyrrol-1-yl, pyrazol-1-yl, etc.; R1 = Ph, 2-MeC6H4, 4-FC6H4, etc.] from aromatic aldehydes, DMSO and azoles was reported. The scope of aldehydes and amides for preparation of enamides I [Ar = Ph, 4-ClC6H4, 4-tBuC6H4, etc.; n = 1, 2] was also reported. In this strategy, DMSO was involved in the construction of the C=C bond as a terminal carbon synthon. Both aromatic aldehydes and azoles could be well tolerated and gave the corresponding terminal N-vinylazoles in 52-91% yields. Based on preliminary experiments, a plausible mechanism was proposed. The experimental process involved the reaction of Oxetan-3-ol(cas: 7748-36-9Computed Properties of C3H6O2)

Oxetan-3-ol(cas: 7748-36-9) is used as a reagent in the synthesis of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. It is also used as a reagent in the synthesis of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors.Computed Properties of C3H6O2

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Formula: C3H6O2In 2022 ,《Visible-Light-Induced [2+2+1] Dearomative Cascade Cyclization of Indole/Furan Alkynes to Synthesize Sulfonyl Polycycles》 was published in Advanced Synthesis & Catalysis. The article was written by Luo, Jiajun; Zeng, Guohui; Cao, Xiaohui; Yin, Biaolin. The article contains the following contents:

Herein, authors report a visible-light-induced [2+2+1] dearomative cascade cyclization of indole/furan alkynes with NaHSO3, providing an array of diverse highly strained sulfonyl polycycles. Compared to authors previous work, this method does not require the use of addnl. sacrificial oxidants and have wider reaction scope. Preliminary mechanistic studies suggest that the indole moiety initiated the reaction, which proceeded via single-electron oxidation pathway. An alkenyl radical formed by intramol. addition capture SO2, and the resulting species is cyclized to furnish the final product. Also, DFT calculations disclosed that the groups on the indole ring or at the side chain probably affect the single electron distribution at the reaction site of IM-RC-I, and the distribution may be a decisive factor of spirocyclization. The experimental part of the paper was very detailed, including the reaction process of Oxetan-3-ol(cas: 7748-36-9Formula: C3H6O2)

Oxetan-3-ol(cas: 7748-36-9) is used as a reagent in the synthesis of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. It is also used as a reagent in the synthesis of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors.Formula: C3H6O2

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Alcohols – Chemistry LibreTexts

Category: alcohols-buliding-blocksIn 2021 ,《Main-Side Chain Hydrogen Bonding-Based Self-Healable Polyurethane with Highly Stretchable, Excellent Mechanical Properties for Self-Healing Acid-Base Resistant Coating》 was published in Macromolecular Rapid Communications. The article was written by Xu, Heng; Tu, Jing; Li, Pingyun; Liang, Li; Ji, Jie; Xiang, Guifeng; Li, Haozhe; Zhang, Yang; Guo, Xiaode. The article contains the following contents:

Developing an autonomous self-healing polyurethane (PU) elastomer with excellent mech. properties and high ductility has attracted increasing attention. Nowadays, the synthesis of elastomers with excellent mech. properties and rapid self-healing at room temperature faces a huge challenge. Herein, This work reports a new supramol. PU with excellent mech. properties and rapid self-healing at room temperature through the introduction of T-type chain extender into the supramol. polymer chain. The introduction of T-chain extender can be used to enhance the mech. strength of PU, and the multiple hydrogen bonds on the side-chain provide theor. support for the rapid self-healing ability of PU. Maximum stress of the synthesized PU can reach 3.4 ± 0.15 Mpa, and maximum elongation at break can reach 3200% ± 160%. Due to flexibility and re-constructibility of side-chain hydrogen bonds, PU stress repair efficiency can reach 96.7%, and can be self-healing scratches rapidly and effectively at room temperature The mech. properties and self-healing properties of PU can be adjusted by the content of T-type chain extender. The PU is applied to the metal surface coating, which has excellent acid-base resistance, bond strength up to 2.9 ± 0.1 Mpa, and the ability to eliminate local damage on the coating surface quickly at room temperature In addition to this study using 2-Aminopropane-1,3-diol, there are many other studies that have used 2-Aminopropane-1,3-diol(cas: 534-03-2Category: alcohols-buliding-blocks) was used in this study.

2-Aminopropane-1,3-diol(cas: 534-03-2) belongs to anime.Typically the presence of an amine functional group is deduced by a combination of techniques, including mass spectrometry as well as NMR and IR spectroscopies. 1H NMR signals for amines disappear upon treatment of the sample with D2O. In their infrared spectrum primary amines exhibit two N-H bands, whereas secondary amines exhibit only one.Category: alcohols-buliding-blocks

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Reference of 4-Aminobutan-1-olIn 2021 ,《High-throughput evaluation of polymeric nanoparticles for tissue-targeted gene expression using barcoded plasmid DNA》 appeared in Journal of Controlled Release. The author of the article were Kim, Jayoung; Vaughan, Hannah J.; Zamboni, Camila G.; Sunshine, Joel C.; Green, Jordan J.. The article conveys some information:

Successful systemic gene delivery requires specific tissue targeting as well as efficient intracellular transfection. Increasingly, research laboratories are fabricating libraries of novel nanoparticles, engineering both new biomaterial structures and composition ratios of multicomponent systems. Yet, methods for screening gene delivery vehicles directly in vivo are often low-throughout, limiting the number of candidate nanoparticles that can be investigated. Here, we report a comprehensive, high-throughput method to evaluate a library of polymeric nanoparticles in vivo for tissue-specific gene delivery. The method involves pairing each nanoparticle formulation with a plasmid DNA (pDNA) that harbors a unique nucleotide sequence serving as the identifying “”barcode””. Using real time quant. PCR (qPCR) for detection of the barcoded pDNA and quant. reverse transcription PCR (RT-qPCR) for transcribed barcoded mRNA, we can quantify accumulation and transfection in tissues of interest. The barcode pDNA and primers were designed with sufficient sensitivity and specificity to evaluate multiple nanoparticle formulations per mouse, improving screening efficiency. Using this platform, we evaluated the biodistribution and transfection of 8 i.v. administered poly(beta-amino ester; PBAE) nanoparticle formulations, each with a PBAE polymer of differential structure. Significant levels of nanoparticle accumulation and gene transfection were observed mainly in organs involved in clearance, including spleen, liver, and kidneys. Interestingly, higher levels of transfection of select organs did not necessarily correlate with higher levels of tissue accumulation, highlighting the importance of directly measuring in vivo transfection efficiency as the key barcoded parameter in gene delivery vector optimization. To validate this method, nanoparticle formulations were used individually for luciferase pDNA delivery in vivo. The distribution of luciferase expression in tissues matched the transfection anal. by the barcode qPCR method, confirming that this platform can be used to accurately evaluate systemic gene delivery. In the experimental materials used by the author, we found 4-Aminobutan-1-ol(cas: 13325-10-5Reference of 4-Aminobutan-1-ol)

4-Aminobutan-1-ol(cas: 13325-10-5) is used in the synthesis of NSAIDs with anti-inflammatory properties. Also used in the synthesis of polyamine transport ligands with specificity against human cancers allowing easy access to specific cancer cells.Reference of 4-Aminobutan-1-ol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Application of 534-03-2In 2021 ,《Machine-learning-assisted low dielectric constant polymer discovery》 appeared in Materials Chemistry Frontiers. The author of the article were Liang, Jiechun; Xu, Shangqian; Hu, Linfeng; Zhao, Yu; Zhu, Xi. The article conveys some information:

Machine learning (ML) has excellent potential for mol. property prediction and new mol. discovery. However, real-world synthesis is the most vital part of determining a polymer’s value. This paper demonstrates automatic polymer discovery through ML and an intelligent cloud laboratory to find new environmentally friendly polymers with low dielec. constants that have potential applications in high-speed communication networks. In the machine learning discovery, we use ML on SMILES from databases to identify ideal functional groups with reasonable solutions Moreover, the solutions are sent to the cloud and synthesized via our intelligent system. A few of them can be successfully synthesized and two of them have excellent performance in low-dielec.-constant applications. This autonomous system enables reliable and efficient combinations of data-driven research and synthesis, reduces both the time and cost of polymer-discovery experiments, and accelerates the overall process for low-dielec.-constant polymer discovery. In the experimental materials used by the author, we found 2-Aminopropane-1,3-diol(cas: 534-03-2Application of 534-03-2)

2-Aminopropane-1,3-diol(cas: 534-03-2) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Application of 534-03-2

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Alcohol – Wikipedia,
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