PrecisION TM hERG-HEK - Nanion Technologies Gmbh
PrecisION TM hERG-HEK - Nanion Technologies Gmbh
PrecisION TM hERG-HEK - Nanion Technologies Gmbh
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NPC - certified cells<br />
<strong>Nanion</strong> NPC-certified cells.<br />
The optimum choice for your assays.<br />
<strong>PrecisION</strong> <strong>TM</strong> <strong>hERG</strong>-<strong>HEK</strong><br />
Cells from Merck Millipore, optimized for <strong>Nanion</strong> Patch Clamp Devices<br />
(NPC) Port-a-Patch, Patchliner and SyncroPatch96.<br />
• Assay optimized for <strong>Nanion</strong> APCs<br />
• Giga Ohm seals<br />
• High success rates<br />
• Stable current responses<br />
• Cell line and assay support<br />
• Optimized patch clamp solutions<br />
NPC - certified cells<br />
See www.nanion.de for more <strong>Nanion</strong> approved cells.
<strong>Nanion</strong> Europe<br />
info@nanion.de<br />
phone +49 89 218997972<br />
www.nanion.de<br />
<strong>Nanion</strong> NPC-certified <strong>hERG</strong>-<strong>HEK</strong> cells<br />
The <strong>hERG</strong> gene (KCNH2) encodes a K + ion channel<br />
responsible for the repolarizing IKr current in the cardiac<br />
action potential. Given the importance of this channel in<br />
maintaining cardiac function, it has become an important<br />
target in compound safety screening.<br />
Compounds can display different properties or different<br />
potencies at physiological temperature (35°C) vs. room<br />
temperature (RT). Therefore, it is of advantage to be able<br />
to study this channel electrophysiologically at elevated<br />
temperature as shown below.<br />
A B<br />
Control<br />
100 µM<br />
Erythromycin<br />
200 pA<br />
200 ms<br />
A <strong>hERG</strong> inhibition of Erythromycin at 35°C as recorded in <strong>hERG</strong>-<strong>HEK</strong> cells. B CRCs for<br />
erythromycin at room temperature and at 35°C. Erythromycin is approximately 10-fold<br />
more potent at 35°C compared with RT. Recordings were done on a Patchliner.<br />
<strong>hERG</strong>-<strong>HEK</strong> from Merck Millipore<br />
<strong>Nanion</strong> <strong>Technologies</strong> GmbH<br />
Erzgiessereistr. 4<br />
80335 Munich, Germany<br />
<strong>Nanion</strong> USA<br />
info@naniontech.com<br />
phone 1-888-9-NANION<br />
www.naniontech.com<br />
Inhibition<br />
Passage stability: > 30<br />
<strong>Nanion</strong> China<br />
info@nanion.cn<br />
phone +86 1082176386<br />
www.nanion.cn<br />
Current amplitude / cell: 919 ± 57 pA (n=54)<br />
phone +49 89 218997972<br />
fax +49 89 218997960<br />
www.nanion.de • info@nanion.de<br />
Raw data traces and CRCs as obtained from <strong>hERG</strong> expressing <strong>hERG</strong>-<strong>HEK</strong> cells.<br />
IC 50 s: Astemizole, IC 50 =1.5 nM (n=34); Propafenone<br />
IC 50 =270 nM (n=15); Quinidine IC 50 =408 nM<br />
(n=16); Terfenadine IC 50 =9.1 nM (n=25); Cisapride<br />
IC 50 =38.5 nM (n=23); E4031 IC 50 =45.5<br />
nM (n=6); Flunarizine, IC 50 =163.7 ± 19 nM (n=3)<br />
Erythromycin IC 50 @ RT= 427.5 µM (n=12),<br />
Erythromycin IC 50 @ 35°C = 30.7 µM (n=18);<br />
Seal resistance: 1.3 ± 0.7 GΩ<br />
CSlow: 7.0 ± 1 pF (n=16)<br />
Rs: 7.5 ± 1 (n=16)<br />
Cell stability after harvesting: ~ 4 hrs<br />
Average whole cell stability: ~ 45 min<br />
Successful whole cell recordings: 70 - 90 %<br />
RT<br />
35ºC<br />
Application directly from frozen stock: yes<br />
1.0<br />
0.8<br />
0.6<br />
0.4<br />
0.2<br />
0.0<br />
0.1 1 10 100 1000<br />
Conc Erythromycin (µM)<br />
Astemizole<br />
3nM Quinidine<br />
300nM<br />
1µM<br />
3µM<br />
10µM<br />
250 ms 250 ms<br />
Propafenone<br />
NPC-certified cells. The optimum choice.<br />
100 pA<br />
inhibition<br />
1<br />
250 ms<br />
IC 50 = 1.5 ± 0.3 nM<br />
(n=34)<br />
10pM<br />
1nM<br />
3nM<br />
10nM<br />
30nM<br />
0<br />
0.0010.01 0.1 1 10 100 1000<br />
Astemizole (nM)<br />
Terfenadine<br />
250 pA<br />
inhibition<br />
1<br />
30pM<br />
3nM<br />
10nM<br />
30nM<br />
100nM<br />
200 pA<br />
inhibition<br />
1<br />
IC 50 = 270 ± 35 nM<br />
(n=15)<br />
0<br />
0.0010.01 0.1 1 10 100<br />
Propafenone (nM)<br />
Cisapride<br />
100pM<br />
10nM<br />
30nM<br />
100nM<br />
300nM<br />
500 pA<br />
inhibition<br />
1<br />
IC 50 = 408 ± 45 nM<br />
(n=16)<br />
3nM<br />
300nM<br />
1µM<br />
3µM<br />
10µM<br />
0<br />
0.0010.01 0.1 1 10 100<br />
Quinidine (nM)<br />
E4031<br />
250 ms 250 ms 250 ms<br />
IC 50 9.1 ± 1.8 nM<br />
(n=25)<br />
250 pA<br />
inhibition<br />
1<br />
IC 50 = 38.5 ± 9 nM<br />
(n= 23)<br />
100pM<br />
10nM<br />
30nM<br />
100nM<br />
300nM<br />
0<br />
0<br />
0<br />
0.01 0.1 1 10 100 1000<br />
Terfenadine (nM)<br />
0.1 1 10 100 100010000<br />
Cisapride (nM)<br />
0.1 1 10 100 100010000<br />
E4031 (nM)<br />
100 pA<br />
inhibition<br />
1<br />
IC 50 = 45.5 ± 7 nM<br />
(n= 6)