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3,4-Difluorobenzyl(1-ethyl-5-(4-((4-hydroxypiperidin-1-yl)-methyl)thiazol-2-yl)-1H-indol-3-yl)carbamate (NAI59), a small molecule with outstanding therapeutic effectiveness to anti-pulmonary fibrosis, was developed as an autotaxin inhibitor candidate compound. To evaluate the pharmacokinetics and plasma protein binding of NAI59, a UPLC–MS/MS method was developed to quantify NAI59 in plasma and phosphate-buffered saline. The calibration curve linearity ranged from 9.95 to 1990.00 ng/mL in plasma. The accuracy was −6.8 to 5.9%, and the intra- and inter-day precision was within 15%. The matrix effect and recovery, as well as dilution integrity, were within the criteria. The chromatographic and mass spectrometric conditions were also feasible to determine phosphate-buffered saline samples, and it has been proved that this method exhibits good precision and accuracy in the range of 9.95–497.50 ng/mL in phosphate-buffered saline. This study is the first to determine the pharmacokinetics, absolute bioavailability, and plasma protein binding of NAI59 in rats using this established method. Therefore, the pharmacokinetic profiles of NAI59 showed a dose-dependent relationship after oral administration, and the absolute bioavailability in rats was 6.3%. In addition, the results of protein binding showed that the combining capacity of NAI59 with plasma protein attained 90% and increased with the increase in drug concentration.  相似文献   
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A graphic sequence π =(d1, d2,..., dn) is said to be forcibly k-edge-connected if every realization of π is k-edge-connected. In this paper, we obtain a new sufficient degree condition for π to be forcibly k-edgeconnected. We also show that this new sufficient degree condition implies a strongest monotone degree condition for π to be forcibly 2-edge-connected and a conjecture about a strongest monotone degree condition for π to be forcibly 3-edge-connected due to...  相似文献   
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在砂土地层中,串囊式充气锚杆的研究还比较少,其承载特性及受力机理尚不明确。本文基于莫尔-库仑模型和Vesic圆孔扩张理论法,分别对圆柱体、球体、组合体、椭球体假设下的串囊式充气锚杆的扩大段进行计算分析。并将计算结果与试验得到的实测值进行对比。结果表明:四种形状假设中椭球体的形状假设理论值与实测值的误差最小,仅为8.35%。通过拟合试验数据,并引入与端阻力和侧摩阻力有关的两个系数对承载力公式进行修正,得到了抗拔承载力的经验公式。  相似文献   
5.
Gao  Zhigen  Guo  Jianhua  Ma  Yanyuan 《中国科学 数学(英文版)》2021,64(8):1905-1916
Science China Mathematics - Linear factor models are familiar tools used in many fields. Several pioneering literatures established foundational theoretical results of the quasi-maximum likelihood...  相似文献   
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Incorporating nanoscale Si into a carbon matrix with high dispersity is desirable for the preparation of lithium-ion batteries (LIBs) but remains challenging. A space-confined catalytic strategy is proposed for direct superassembly of Si nanodots within a carbon (Si NDs⊂C) framework by copyrolysis of triphenyltin hydride (TPT) and diphenylsilane (DPS), where Sn atomic clusters created from TPT pyrolysis serve as the catalyst for DPS pyrolysis and Si catalytic growth. The use of Sn atomic cluster catalysts alters the reaction pathway to avoid SiC generation and enable formation of Si NDs with reduced dimensions. A typical Si NDs⊂C framework demonstrates a remarkable comprehensive performance comparable to other Si-based high-performance half LIBs, and higher energy densities compared to commercial full LIBs, as a consequence of the high dispersity of Si NDs with low lithiation stress. Supported by mechanic simulations, this study paves the way for construction of Si/C composites suitable for applications in future energy technologies.  相似文献   
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In the paper, the authors establish several integral representations for the generating functions of the large and little Schröder numbers and for the large and little Schröder numbers.  相似文献   
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In this communication, we report the synthesis of small‐sized (<10 nm), water‐soluble, magnetic nanoparticles (MNPs) coated with polyhedral oligomeric silsesquioxanes (POSS), which contain either polyethylene glycol (PEG) or octa(tetramethylammonium) (OctaTMA) as functional groups. The POSS‐coated MNPs exhibit superparamagnetic behavior with saturation magnetic moments (51–53 emu g?1) comparable to silica‐coated MNPs. They also provide good colloidal stability at different pH and salt concentrations, and low cytotoxicity to MCF‐7 human breast epithelial cells. The relaxivity data and magnetic resonance (MR) phantom images demonstrate the potential application of these MNPs in bioimaging.  相似文献   
10.
JPC – Journal of Planar Chromatography – Modern TLC - A new high-performance thin-layer chromatographic (HPTLC) method has been developed for the simultaneous estimation of...  相似文献   
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