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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)

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