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. 2005 Aug 15;202(4):517–527. doi: 10.1084/jem.20050119

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Copyright © 2005, The Rockefeller University Press

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Figure 1. — Characteristics of the 11β-HSD1 inhibitor compound 544. (A) Structure and in vitro potency of compound 544. Potency of compound 544 against human and murine 11β-HSD1 and -HSD2 was determined as described in Materials and methods. The IC₅₀ was determined from >25 determinations for each enzyme. (B) PD activity of 11β-HSD1 inhibitor in serum. Compound 544 was orally administered to mice and the percent inhibition of [³H]cortisone conversion to cortisol was measured relative to controls dosed with vehicle only. Data are a representative study of at least two experiments. Statistical significance is calculated between the treatment groups and vehicle controls (*, P < 0.05; **, P < 0.005). Values represent the mean ± SEM. (C) PD activity of 11β-HSD1 inhibitor in key organs. Data are the mean of two experiments. Statistical significance is calculated between the treatment groups and vehicle controls (*, P < 0.05; **, P < 0.005). Values represent the mean ± SEM.