A Dual Inhibitor of DYRK1A and GSK3β for β-Cell Proliferation: Aminopyrazine Derivative GNF4877

Loss of β-cell mass and function can lead to insufficient insulin levels and ultimately to hyperglycemia and diabetes mellitus. The mainstream treatment approach involves regulation of insulin levels; however, approaches intended to increase β-cell mass are less developed. Promoting β-cell proliferation with low-molecular-weight inhibitors of dual-specificity tyrosine-regulated kinase 1A (DYRK1A) offers the potential to treat diabetes with oral therapies by restoring β-cell mass, insulin content and glycemic control. GNF4877, a potent dual inhibitor of DYRK1A and glycogen synthase kinase 3β (GSK3β) was previously reported to induce primary human β-cell proliferation in vitro and in vivo. Herein, we describe the lead optimization that lead to the identification of GNF4877 from an aminopyrazine hit identified in a phenotypic high-throughput screening campaign measuring β-cell proliferation.     

Photovoltaic Power Supply Unit for the Basic Stations of Cellular Companies

The data on the use of solar photovoltaic plants (PVPs) for providing a reliable and guaranteed power supply to telecommunication systems and cellular communication systems in the conditions prevalent in Uzbekistan are given. The research-based structures developed by OOO MIR SOLAR and the selection of PVP elements ensuring their reliable operation are described. The main influencing factors are discussed, and the use of effective combinations of different types of panels (from monocrystalline and polycrystalline silicon) and a specially developed controller are considered.     

Carbon supported bimetallic Ru‐Co catalysts for H2 production through NaBH4 and NH3BH3 hydrolysis

This work investigates the effect of the addition of small amounts of Ru (0.5‐1 wt%) to carbon supported Co (10 wt%) catalysts towards both NaBH₄ and NH₃BH₃ hydrolysis for H₂ production. In the sodium borohydride hydrolysis, the activity of Ru‐Co/carbon catalysts was sensibly higher than the sum of the activities of corresponding monometallic samples, whereas for the ammonia borane hydrolysis, the positive effect of Ru‐Co systems with regard to catalytic activity was less evident. The performances of Ru‐Co bimetallic catalysts correlated with the occurrence of an interaction between Ru and Co species resulting in the formation of smaller ruthenium and cobalt oxide particles with a more homogeneous dispersion on the carbon support. It was proposed that Ru^°, formed during the reduction step of the Ru‐Co catalysts, favors the H₂ activation, thus enhancing the reduction degree of the cobalt precursor and the number of Co nucleation centers. A subsequent reduction of cobalt and ruthenium species also occurs in the hydride reaction medium, and therefore the state of the catalyst before the catalytic experiment determines the state of the active phase formed in situ. The different relative reactivity of the Ru and Co active species towards the two investigated reactions accounted for the different behavior towards NaBH₄ and NH₃BH₃ hydrolysis.     

The Role of Excitation Photons Energy in the Photoinduced Carrier Dynamics in InGaAs/InAlAs Superlattice Heterostructures

Technical Physics Letters - The influence of excitation photons energy on the relaxation times of photoexcited carriers is studied. The involved relaxation mechanisms are evaluated and the...     

Peculiarities of Monitoring the State of a Flowing Medium by the Method of Nuclear Magnetic Resonance

Technical Physics Letters - Specific features of monitoring the state of a flowing medium by method of nuclear magnetic resonance (NMR) are considered. An approach to studying the state of a...     

Influence of the Chemical Composition and Local Atomic Packing of Nanostructured MoSx and MoSex Solid Lubricant Coatings on Their Tribological Properties under Complicated Conditions

Technical Physics Letters - We present the results of a comparative investigation of the friction and wear characteristics of MoSx and MoSex coatings in an oxidizing medium (argon–air...     

Detailed study on fusion characteristics of rigid poly(vinyl chloride) nanocomposites: The comparison of using multiple regression analysis and artificial neural network

Fusion behavior of poly(vinyl chloride) (PVC) compounds plays an important role in the development of physical properties of processed material. The fusion characteristics in PVC processing are governed by material variables that affect the fusion with some interactions. In this research, the aim was to characterize the effects of formulation ingredients on fusion characteristics of PVC. Four material parameters, including the contents of nanoclay (NC), azodicarbonamide, calcium stearate, and processing aid, are proposed as affecting variables. The fusion time (FT) as well as fusion factor (FF) are considered fusion indicators and are experimentally determined in some different levels of affecting parameters. The multivariable regression analysis (MRA) and the Artificial Neural Network (ANN) modeling are considered as two analytical methods. The regression analysis result for the FT denotes, in part, significant linear and quadratic effects of NC and also its significant interactions with azodicarbonamide and calcium stearate, whereas that of FF indicates only a linear effect of NC. ANN modeling is performed with a three‐layer (input, hidden, and output) neural network. The results of the comparison of the MRA and ANN predictions with experimental values are reported as the correlation coefficient (R²), mean‐square error, and mean absolute percentage error for both FF and FT parameters. The obtained values clearly denote that the ANN results are more precise and especially more general than those of MRA. However, in the case of FT, improvement of the ANN modeling is much greater than that of FF. J. VINYL ADDIT. TECHNOL., 21:147–155, 2015. © 2014 Society of Plastics Engineers     

Phase-Structural and Electrochemical Properties of La2MgNi9 Alloys

Powder Metallurgy and Metal Ceramics - Multiphase La 2 MgNi 9 alloys are synthesized by induction melting. The crystalline structures of all phases in the alloys are determined with X-ray...     

Effect of an abrupt change in pulling rate on microstructures of directionally solidified Al2O3-Er3Al5O12 eutectic and off-eutectic composite ceramics

Directionally solidified microstructures of Al₂O₃-Er₃Al₅O₁₂ eutectic and off-eutectic in situ composite ceramics were explored under abrupt-change pulling rate conditions. Corresponding temperature distributions and interface locations were studied. In eutectic composition, fluctuation of eutectic spacing occurred when the pulling rate increased abruptly. A gradually increase or abrupt increase in eutectic spacing was observed when the pulling rate decreased abruptly. In hypoeutectic and hypereutectic compositions, formation of the primary phases were suppressed when the pulling rate increased abruptly from 10?µm/s to 100?µm/s, while primary phases precipitated when the pulling rate decreased abruptly from 100?µm/s to 10?µm/s. The interface altitude decreased after the pulling rate increased abruptly, but increased after the pulling rate decreased abruptly. The liquid composition restriction (around the eutectic composition) at the eutectic interface plays an important role in the suppression of the primary dendrite and coupled eutectic oxides can be obtained in off-eutectic compositions even under higher solidification rate conditions.