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lumacaftor Generally replacement of the aryl group
2021-10-01
Generally, replacement of the aryl group was well tolerated, with tetrahydropyran () and hydroxyl () functionality providing potency equivalent to and . These substitutions had no effect on selectivity versus GlyT2 and taurine transporter (TauT)—no activity was observed at micromolar concentrations
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br Materials and methods br Results br Discussion
2021-10-01
Materials and methods Results Discussion l-glutamate is the major excitatory neurotransmitter in the brain, and is functionally involved in many processes of the nervous system which have been connected with several neurological diseases [4]. These conditions are characterized by the time-d
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br Conclusion In conclusion SHP was demonstrated as a potent
2021-10-01
Conclusion In conclusion, SHP289-04 was demonstrated as a potent glucokinase activator. It could normalize the blood glucose level and lipid level in spontaneous type 2 diabetes model KKAy mice. At the same time, it ameliorated the function of islets and liver in KKAy mice. It had been proved to
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During the activation of the coagulation
2021-09-30
During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium BMS-754807 on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit plat
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The newly synthesized compounds were evaluated for their
2021-09-30
The newly synthesized compounds were evaluated for their FAAH inhibitory activity in vitro. In addition, molecular modeling, selectivity and reversibility behavior of the new class of FAAH inhibitors are presented in this article. Results and discussion The potency of inhibition on the human rec
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The concentration of rapamycin that gave
2021-09-30
The concentration of rapamycin that gave half-maximal induction of the expression of HO-1 and Prx-1 mRNA in normal hepatocytes was 0.05 μM, with maximal induction at about 0.1 μM rapamycin. While, at rapamycin concentrations higher than 0.1 μM, the degree of enzyme induction decreased, elevated expr
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Preadipocytes are capable of differentiating into lipid lade
2021-09-30
Preadipocytes are capable of differentiating into lipid-laden mature adipocytes. Lipid droplets are a prominent morphological feature of mature adipocytes, which is accumulated and maintained during adipocytes differentiation [26]. In this study, rHhip treatment increased lipid accumulation, as well
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cholesterol absorption inhibitors Platycodon grandiflorum is
2021-09-30
Platycodon grandiflorum is a member of the genus Platycodon and is commonly known as balloon flower. In East Asia, P. grandiflorum is used for the treatment of asthma, coughs, inflammatory diseases, pulmonary tuberculosis, and diabetes (Takagi and Lee, 1972). Furthermore, recent studies have report
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Among the compounds prepared at
2021-09-30
Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with modera
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br Methods br Results Top panels of the Fig show
2021-09-30
Methods Results Top panels of the Fig. 1 show the conventional representation of the predicted values of TL,CO according to ERS’93 and GLI′17 as a function of age and keeping the height constant (160 cm, panel A and 190 cm, panel B). This figure shows that the GLI-‘17 predicted values of TL,CO
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br Conclusion br Acknowledgment This
2021-09-30
Conclusion Acknowledgment This study was supported by grants from the Excellence Initiative of the German federal and state governments, the Else Kröner-Fresenius Foundation and the German Society for Cardiology (DGK) to F.K. and grants from the Deutsche Forschungsgemeinschaft (SFB TRR 219 M-0
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br Acknowledgments br Introduction When
2021-09-30
Acknowledgments Introduction When human red blood cell (hRBC) membranes are depolarized, either as intact SR 1664 suspended in depolarizing (low Cl−) Ringers or under voltage clamp conditions using excised inside-out patches, they respond by opening a nonselective voltage-dependent cation (NS
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The GH family has potential applications in various industri
2021-09-30
The GH family has potential applications in various industries. A putative ORF encoding α-galactosidase, namely GalR, with a low identical match and e-value and high query coverage in the metagenome was selected because it demonstrated considerable activity. GalR shared 65% identity with the GH 27 p
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Occupying at least of brain volume astroglial cells not
2021-09-29
Occupying at least 50% of GW5074 volume, astroglial cells not only possess a high level of association in network through gap junctions and direct intercellular communications [28], but also are extensively exposed to extracellular fluid and contribute in shaping different types of synapses [29]. Ou
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br Characterization of quantal exocytosis by amperometry A s
2021-09-29
Characterization of quantal exocytosis by amperometry A secretory vesicle experiences four phases during exocytosis: (i) cargo packaging & translocation, (ii) vesicle docking & priming; (iii) fusion pore formation; (iv) fusion pore expansion and cargo secretion (Fig. 1a). The release of monoamine
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