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. 2016 Mar 15;6(3):e760. doi: 10.1038/tp.2016.13

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Copyright © 2016 Macmillan Publishers Limited

This work is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License. The images or other third party material in this article are included in the article's Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by-nc-sa/4.0/

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Activity of carbenoxolone (CBX, 18β-glycyrrhetinic acid 3β-O-hemisuccinate) and αCBX (18α-glycyrrhetinic acid 3β-O-hemisuccinate) on mouse and human 11β-HSD1 and 11β-HSD2. We tested the IC50 of 18α−18β-glycyrrhetinic acid 3β-O-hemisuccinate against human and mouse 11β-HSD1 and 11β-HSD2 by means of homogeneous time-resolved fluorescence (HTRF) assays. (a and c) CBX yielded IC50 values of 753.1 nm for human 11β-HSD1 and 4.62 μm for mouse 11β-HSD1. (b and d) CBX yielded IC50 values of 379.6 nm for human 11β-HSD2 and 628.7 nm for mouse 11β-HSD2. (e and g) αCBX yielded IC50 values of 15.92 μm for human 11β-HSD1 and 48.25 μm for mouse 11β-HSD1. (f and h) αCBX yielded IC50 values of 30.67 μm for human 11β-HSD2 and 1.06 μm for mouse 11β-HSD2. Results for CBX are the average of two to three independent replicates; results for αCBX are the average of three to four independent replicates.