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The most potent probe, [18F]9a, exhibited a combination of high binding affinity to Aβ aggregates (Ki = 21.0 ± 4.9 nM), high initial brain uptake (9.14% ID/g at 2 min), fast clearance from normal brain tissue (1.79% ID/g at 60 min), and satisfactory in vivo biostability in the brain (95% of intact form at 2 min).
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As labeling in PBS does not reflect the conditions of the growth inhibition experiments (Fig. 2) we investigated the cell permeability and target binding of the most potent probes ACV1 and ACV2 under cell culture conditions with incubation of up to several days.
Validation of dual enzyme targeting through activity-based proteome profiling with an alkyne probe modeled after the most potent inhibitor, and preliminary serum stability studies of selected derivatives are also described.
One compound, called Probe 8, proved to be the most potent in a pull-down assay and demonstrated a TIR1-dependent auxin-antagonistic response in Arabidopsis thaliana.
We observed that each of the peptolide probes retained potent prokaryotic translation inhibition, although the most potent peptolide, 12b, is almost equipotent as TE-802 and 2.0-fold less active than 1, the positive ketolide and macrolide controls, respectively.
Numerous analogues were synthesized to investigate SAR at three regions of the scaffold leading to a more potent fluorinated biaryl nitrile 4. Compound 4 was the most potent in the whole cell assays for inhibition of pyoverdine production directly measured by HPLC and has been designated as Probe Compound ML318.
Instead he became its most potent critic.
Height is our most potent architectural currency.
"Which one is the most potent?
"Bananas are a most potent source".
Whose patent portfolio is most potent?
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CEO of Professional Science Editing for Scientists @ prosciediting.com