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