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. 2013 Dec 21;7:1–14. doi: 10.2147/DMSO.S50209

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© 2014 Zambad et al. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License

The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

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Activation of TGR5 by TRC210258. (A) Effect of TRC210258 on TGR5-mediated cAMP formation. EC₅₀ value expressed in nM. (B) Effect of TRC210258 on CRE luciferase reporter. EC₅₀ value expressed in nM. (C) Effect of TRC210258 on GLP1 secretion from NCI-H716, a human enteroendocrine cell line. GLP1 levels expressed in pM. Each value is the average of two experiments, each performed in duplicate. *P<0.05, TRC210258 versus vehicle control.

Abbreviations: DMSO, dimethyl sulfoxide; TRC210258, N-(4-chlorophenyl)-2-(4-fluorophenoxy)-N-methylimidazo [1, 2-a] pyrimidine-3-carboxamide; GLP, glucagon like peptide 1; CRE, cyclic AMP responsive element; pM, picomole; conc, concentration.