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PK inhibits KCNH2. 3 / 3
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"Our present study revealed that while PK cleaves hERG at the S5-S6 linker and abolishes I hERG, it cleaves Kv1.5 at the S1-S2 linker and does not decrease I Kv1.5."
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"However, due to differences between hERG and Kv1.5 in terms of their three extracellular linkers (length, sequence, and 3D structure), PK cleaves hERG in the S5-S6 linker and eliminates I hERG, wherea[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"YCT-529 did not inhibit the cardiac hERG ion channel, was not toxic for HepG2 and lung fibroblast cells, and showed neither mutagenic (Ames assay) nor genotoxic (chromosomal aberration and rat micronucleus studies) potential.Given the favorable characteristics of YCT-529, we determined its in vivo oral bioavailability and pharmacokinetic (PK) properties in plasma, brain and testes of male CD-1 mice (6–8 weeks, 30–35 g)."
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