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ICA-105574 activates KCNH2. 7 / 7
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"The highest final concentration of DMSO in external solution was 0.1%, a concentration that had no effect on hERG current, APD and ECG parameters.Previous studies have demonstrated that both ICA-10557[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
24041920
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"ICA-105574 (ICA), a 3-Nitro-n-(4-phenoxyphenyl) benzamide derivative activates hERG1 by strongly attenuating pore-type inactivation."
31877041
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"First, we validated in vivo the ability of ICA-105574 to rescue QT prolongation in a sotalol-induced animal model mimicking LQT2."
40197385
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"It had been previously established by experiment that PD-118057 and ICA-105574, drugs that inhibits inactivation and thus increase hERG current, bind near F619 and L622 XREF_BIBR, XREF_BIBR."
22848423
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"In the studied HERG mutations, suppression of the tail currents made it impossible to accurately calculate the activation curve parameters, including the half-activation voltage (V ) and the slope factor (κ), which are necessary to evaluate the voltage dependence of HERG channel activation induced by the mutations (as in Sanguinetti et al. for A561V and G628S [62]) and by ICA-105574."
40197385
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"The primary mechanism by which ICA-105574 potentiates hERG channel activity is by removing hERG channel inactivation, because ICA-105574 (2 microM) shifts the midpoint of the voltage-dependence of inactivation by> 180 mV from -86 to +96 mV."
19805508
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"ICA-105574 increases outward hERG1 currents (EC 50 of 0.5 muM, Hill slope of 3.3) far more than any other known agonist [XREF_BIBR]."
24721650