Structures and activity in fluorometric assays of HC-070 and HC-608. Stefan Just Bertrand L. Chenard Angelo Ceci Timothy Strassmaier Jayhong A. Chong Nathaniel T. Blair Randall J. Gallaschun Donato del Camino Susan Cantin Marc D’Amours Christian Eickmeier Christopher M. Fanger Carsten Hecker David P. Hessler Bastian Hengerer Katja S. Kroker Sam Malekiani Robert Mihalek Joseph McLaughlin Georg Rast JoAnn Witek Achim Sauer Christopher R. Pryce Magdalene M. Moran 10.1371/journal.pone.0191225.g001 https://plos.figshare.com/articles/figure/Structures_and_activity_in_fluorometric_assays_of_HC-070_and_HC-608_/5843088 <p>The chemical structures of (A) HC-070 and (B) HC-608 (Pico145). (C) Inhibition of hTRPC5 by HC-070 and HC-608 in indicator-assisted calcium influx analysis. Concentrations tested ranged from 1 picomolar (pM) to 1 μM. Each data point represents the average of 8 measurements from a 384-well plate. Error bars show the standard deviation. The IC<sub>50</sub> values were 9.3 ± 0.9 and 6.2 ± 0.5 nanomolar (nM), respectively. (D) Inhibition of hTRPC4 by HC-070 and HC-608 over the same range of concentrations. The IC<sub>50</sub> values were 46.0 ± 3.9 nM and 32.5 ± 1.8 nM, respectively (n = 8). Error bars represent the standard deviation.</p> 2018-01-31 18:38:28 HC -070. HC -070 EPM CCK TRPC 5 channels non-selective cation channels heterologous expression systems HC -070 TRPC 5 TRPC 4 HC -070 ameliorates molecule antagonist HC -070 attenuates TRPC 5 homomultimers channel canonical subfamily IC TRPC 5 mice