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It should be noted that doses of 1 and 10 μg/kg DES induce almost a similar transcriptional activation, and the activation is approximately 20% of maximal activity induced by DES.
To determine if the dose-response curve of estradiol has been altered by the addition of ER-α, the data from Figure 5A is replotted as a percent of the maximal activity induced by a saturating concentration of 17β-estradiol (Fig. 5B).
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The residues Trp83 and Val178 are both conserved in mammals, and the mutations W83R and V178M led to significantly reduced TGR5 response to TLC concentrations (0.1 2.5 µM) close to the concentration known to induce half maximal activity of wild-type TGR5 (0.29 µM) [36].
The maximal FM550-induced activity of 5.7 ± 0.3-fold was less than the activity induced by a maximally efficacious concentration of rosiglitazone (1 μM; 11.3 ± 0.9-fold; EC50 of 0.02 μM; see Supplemental Material, Figure S2A).
While RIF-1 is the only molecule detected with rosette-inducing activity, its maximal activity (5.6 ± 0.5% colonial cells/total cells) differs from that of the sphingolipid-enriched lipid fraction (19.2 ± 4.6% colonial cells/total cells; Figure 4).
In the PPARγ/RXRα Cos7 cell reporter assay, TPP significantly induced PPARγ-driven reporter activity at concentrations ≥ 10 μM, with an EC50 of 8 μM and maximal activity of 7.5 ± 0.7-fold, and ITP significantly induced PPARγ-driven reporter activity at concentrations ≥ 10 μg/mL (30 μM), with an EC50 of 8 μM and maximal activity of 5.1 ± 0.6-fold.
The GGA1 box provides maximal promoter activity, and deletion of the spacer element appears to increase the activity induced by the GGA boxes [35].
Promoter 2 was induced between 6 and 10 hours of development and reached maximal activity between 14 and 16 hours to decrease thereafter.
DMXAA induced similar TNF activity in WT and TNFR1−/− mice, with maximal activity at 75 mg kg−1.
These results demonstrate that a functional TNAP is induced as early as day 3 of both the serotonergic and noradrenergic neuronal pathways and reaches a maximal activity upon implementation of a complete bioaminergic phenotype.
The rearing activity induced by 8-OH-DPAT was attenuated only at a higher dose of galanin within the first 40 min (maximal value F2,21 = 9.374 at 10 min), whereas the lower dose did not differ from the effect of 8-OH-DPAT alone.
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