IndraLab

Statements

Glu-Phe-Val inhibits KCNH2. 6 / 6
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"EFV concentrations exceeding 0.4 mug/mL significantly inhibited outward hERG tail currents (P < 0.05)."
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"The observed concentration-response relationship and the gene-dose effect in the clinical trial coupled with the in vitro demonstration of EFV induced hERG inhibition were important findings to support the observed QTc prolongation in the relatively small number of CYP2B6*6 homozygotes."
27333947
reach
"EFV concentrations exceeding 0.4 microg/mL significantly inhibited outward hERG tail currents (P < 0.05)."
27333947
reach
"The observed concentration response relationship and the gene-dose effect in the clinical trial coupled with the in vitro demonstration of EFV induced hERG inhibition were important findings to support the observed QTc prolongation in the relatively small number of CYP2B6 * 6 homozygotes."
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"EFV also inhibited inward and outward I hERG when applied to the culture media for 24 hours."
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"Most drugs that clinically prolong the QTc interval are inhibitors of the rapid component of the delayed rectifier current which is encoded by the hERG gene. xref A concentration-dependent inhibition of I hERG by EFV was observed with an IC 50 estimated to be approximately 0.2 µg/mL (i.e. unbound EFV IC 50 )."
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