Figure 1. Uptake of relebactam into human OAT1, OAT3 and OCT2 stably transfected cells. Time-dependent uptake of ... Figure 1. Uptake of relebactam into.

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Figure 1. Uptake of relebactam into human OAT1, OAT3 and OCT2 stably transfected cells. Time-dependent uptake of ... Figure 1. Uptake of relebactam into human OAT1, OAT3 and OCT2 stably transfected cells. Time-dependent uptake of relebactam (2 μM) into MDCKII and MDCKII-OAT1 cells (a), MDCKII and MDCKII-OAT3 cells (b), and CHO-K1 and CHO-K1-OCT2 cells (c). Positive controls: uptake of [<sup>3</sup>H]PAH (1 μM) (d), [<sup>3</sup>H]ES (1 μM) (e) and [<sup>14</sup>C]TEA (1 μM) (f) for OAT1, OAT3 and OCT2, respectively, measured at 7 min. Values shown are mean ± SEM of experiments performed in triplicate. **P < 0.01; *P < 0.05. ES, estrone sulphate; PAH, p-aminohippuric acid; SEM, standard error of the mean; TEA, tetraethylammonium. Unless provided in the caption above, the following copyright applies to the content of this slide: © The Author(s) 2019. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For permissions, please email: journals.permissions@oup.com.This article is published and distributed under the terms of the Oxford University Press, Standard Journals Publication Model (https://academic.oup.com/journals/pages/open_access/funder_policies/chorus/standard_publication_model) J Antimicrob Chemother, dkz101, https://doi.org/10.1093/jac/dkz101 The content of this slide may be subject to copyright: please see the slide notes for details.

Figure 2. Uptake of relebactam into human OAT4 transiently transfected HEK293 cells. Time-dependent uptake of ... Figure 2. Uptake of relebactam into human OAT4 transiently transfected HEK293 cells. Time-dependent uptake of [<sup>14</sup>C]relebactam (10 μM) into HEK293 and HEK293-OAT4 cells pretreated with (a) or without 5 mM glutaric acid (d). Uptake in the transfected cell line was significantly different from the parental cell line (P < 0.01). Uptake of [<sup>14</sup>C]relebactam (10 μM) into HEK293 and HEK293-OAT4 cells, pretreated with (b) or without 5 mM glutaric acid (e), in the presence and the absence of probenecid (1 mM) at 15 min. Positive controls: uptake of [<sup>3</sup>H]ES (1 μM) into HEK293 and HEK293-OAT4 cells, pretreated with (c) or without 5 mM glutaric acid (f), in the presence and the absence of probenecid (1 mM) at 15 min. Values shown are mean ± SEM of experiments performed in triplicate. ES, estrone sulphate; SEM, standard error of the mean. Unless provided in the caption above, the following copyright applies to the content of this slide: © The Author(s) 2019. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For permissions, please email: journals.permissions@oup.com.This article is published and distributed under the terms of the Oxford University Press, Standard Journals Publication Model (https://academic.oup.com/journals/pages/open_access/funder_policies/chorus/standard_publication_model) J Antimicrob Chemother, dkz101, https://doi.org/10.1093/jac/dkz101 The content of this slide may be subject to copyright: please see the slide notes for details.

Figure 3. Uptake of [14C]relebactam into human MATE1 and MATE2K stably transfected CHO-K1 and MDCKII cells. ... Figure 3. Uptake of [<sup>14</sup>C]relebactam into human MATE1 and MATE2K stably transfected CHO-K1 and MDCKII cells. Time-dependent uptake of [<sup>14</sup>C]relebactam (10 μM) into CHO-K1 and CHO-K1-MATE1 cells (a), and MDCKII and MDCKII-MATE2K cells (d). Uptake in the transfected cell line was significantly different from that in the parental cell line (P < 0.05). Uptake of [<sup>14</sup>C]relebactam (10 μM) into CHO-K1 and CHO-K1-MATE1 cells in the presence and the absence of control inhibitor quinidine (100 μM) (b), and MDCKII and MDCKII-MATE2K cells in the presence and the absence of control inhibitor pyrimethamine (5 μM) (e) at 20 min. Positive controls: uptake of [<sup>14</sup>C]metformin (5 μM) into CHO-K1 and CHO-K1-MATE1 cells in the presence and the absence of control inhibitor quinidine (100 μM) (c), and MDCKII and MDCKII-MATE2K cells in the presence and the absence of control inhibitor pyrimethamine (5 μM) (f) at 20 min. Values shown are mean ± SEM of experiments performed in triplicate. SEM, standard error of the mean. Unless provided in the caption above, the following copyright applies to the content of this slide: © The Author(s) 2019. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For permissions, please email: journals.permissions@oup.com.This article is published and distributed under the terms of the Oxford University Press, Standard Journals Publication Model (https://academic.oup.com/journals/pages/open_access/funder_policies/chorus/standard_publication_model) J Antimicrob Chemother, dkz101, https://doi.org/10.1093/jac/dkz101 The content of this slide may be subject to copyright: please see the slide notes for details.

Figure 4. Kinetics of OAT3-mediated uptake of relebactam Figure 4. Kinetics of OAT3-mediated uptake of relebactam. (a) Concentration-dependent uptake of relebactam into MDCKII ... Figure 4. Kinetics of OAT3-mediated uptake of relebactam. (a) Concentration-dependent uptake of relebactam into MDCKII and MDCKII-OAT3 cells at 5 min. (b) OAT3-mediated uptake of relebactam at 5 min. Values shown are mean ± SEM of experiments performed in triplicate. SEM, standard error of the mean. Unless provided in the caption above, the following copyright applies to the content of this slide: © The Author(s) 2019. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For permissions, please email: journals.permissions@oup.com.This article is published and distributed under the terms of the Oxford University Press, Standard Journals Publication Model (https://academic.oup.com/journals/pages/open_access/funder_policies/chorus/standard_publication_model) J Antimicrob Chemother, dkz101, https://doi.org/10.1093/jac/dkz101 The content of this slide may be subject to copyright: please see the slide notes for details.