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Most biotinylated squamocin and bullatacin derivatives show similar in vitro cytotoxicity against the biotin receptor non-overexpressed L1210 cells as squamocin and bullatacin, respectively, while against biotin receptor overexpressed 4T1 and P815 tumor cells, several derivatives show significantly higher potency and better selectivity.
In transfected cells that express human or rat CLR/RAMP1, CGRP has significantly higher potency than rAmy (∼250-fold, Fig. 2 and Table 2).
Third, comparing the third-generation triazole derivatives anastrozole and letrozole, letrozole showed a significantly higher potency with respect to aromatase inhibition in breast homogenates and breast fibroblasts [ 52].
In addition, the various parts of the manuscript are not as well connected as they could be (e.g., the discovery of the new erastin analogs with significantly higher potency in Figure 3 are not used in any subsequent experiments).
44 Saxagliptin has the advantage of having a very high selectivity towards DPP-4 and in comparison to sitagliptin and vildaglitpin it has a significantly higher potency to inhibit DPP-4 in vitro.
After incubation, in LPS-stimulated PBMC and in activated LPMC from IBD patients, BXL-62 significantly inhibited, with a significantly higher potency compared with 1,25(OH)2D3, TNF- α, IL-6, and IL-12/23p40 transcription and cytokine concentrations measured in culture supernatants without differences between CD and UC.
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The majority of the tested bivalent and biparatopic VHH constructs had a significantly higher neutralizing potency than the corresponding monovalent VHH, both for CVS-11 and EBLV-1 (Table 5).
The majority of the tested bivalent and trivalent VHH constructs had a significantly higher neutralizing potency than the corresponding monovalent VHH against all four clades of H5N1 tested, with the bivalent and trivalent constructs based on Infl-C8 being the best neutralizers (Table 3).
Consequently, the re-designed rAAVs demonstrated significantly higher biological potencies, even in a comparison with HEK293-manufactured rAAVs mediating, in the case of rAAV5, 4-fold higher transduction of brain tissues in mice.
However, none of these compounds had a potency significantly higher than 1 nmol L−1 in the natural substrate assay.
27 In comparison to the older 5-HT3 receptor antagonists, it has a higher binding affinity to the 5-HT3 recepTable(Table 2), a higher potency, a significantly longer half-life (approximately 40 hours, 4 to 10 times longer than that of dolasetron, granisetron, or ondansetron) (Table 2), and an excellent safety profile as demonstrated in a number of phase II III studies.
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