IndraLab

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NS1643 activates KCNH2. 11 / 11
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"When assessed with 2-s depolarizations, NS1643 enhanced the magnitude of wild-type hERG current in a concentration- and voltage dependent manner with an EC (50) of 10.4 microM at -10 mV."
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"NS1643, a Kcnh2 activator, was applied to activate Kcnh2 for confirming again the role of Kcnh2 in SICD."
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"Casis et al. (11) reported that NS1643 activates hERG channels expressed in Xenopus oocytes in a concentration- and voltage dependent manner and strongly affects channel inactivation by shifting the v[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In this study, we showed that both mallotoxin and NS1643 activated hERG current by 87% and 55% at 3muM, respectively."
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"In the absence of channel inactivation, NS1643 did not enhance hERG current magnitude."
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"Activation of Kcnh2 by NS1643 exhibited opposite outcome, indicating a potential role of the molecule in heart protection during sepsis."
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"Nevertheless, NS1643 then continued to produce concentration- and voltage dependent increases in hERG current amplitude."
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"HERG channels treated with NS1643 behave in a very similar way to WT channels in the absence of NS1643 : following depolarization, NS1643 activated HERG channels inactivate rapidly and recover from inactivation, passing an outward current as the membrane potential recovers."
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"NS1643, which activated hERG current by 55% at 3muM in hERG transfected HEK293 cells, significantly shortened APD and increased coronary flow at 1 and 10muM."
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"Activation of Kcnh2 by NS1643 exhibited opposite outcome , indicating a potential role of the molecule in heart protection during sepsis ."
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"As expected, mallotoxin activated hERG current by 87% at 3muM, and NS1643 activated hERG current by 55% at 3muM."
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