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Cmax in rat administered as repeated dose for 6 days
Assay data:1 Tested
SummaryPubMed Citation
Cmax in rat administered as single dose
Toxicity in rat assessed as NOAEL administered as repeated dose for 6 days
Toxicity in rat assessed as NOAEL administered as single dose
Inhibition of GIRK1/2 (unknown origin) channel
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Brain to plasma ratio in iv dosed rat measured after 30 mins
Equilibrium solubility of the compound at pH 7.4
Apparent permeability across apical to basolateral side in MDCK cells
Assay data:17 Tested
Substrate activity at p-glycoprotein in MDCK cells overexpressing MDR1 assessed as efflux ratio of permeability from basolateral to apical side over apical to basolateral side
Assay data:15 Tested
Inhibition of recombinant hERG in the presence of dofetilide by competitive binding assay
Assay data:4 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of recombinant human KCNQ1
Inhibition of recombinant human Cav1.2
Inhibition of recombinant human Nav1.5
Inhibition of recombinant human GIRK1/4 channel
Assay data:17 Active, 17 Activity ≤ 1 µM, 18 Tested
Toxicity in langendorff-perfused guinea pig heart assessed as effect on left atrial action potential duration at 10 uM
Toxicity in langendorff-perfused guinea pig heart assessed as effect on left ventricular action potential duration at 10 uM
Toxicity in langendorff-perfused guinea pig heart assessed as effect on QT interval at 10 uM
Toxicity in langendorff-perfused guinea pig heart assessed as effect on coronary artery perfusion pressure at 10 uM
Toxicity in langendorff-perfused guinea pig heart assessed as effect on PR interval at 10 uM
Effect on fingolimod-induced shortening of AERP in guinea pig model assessed as prolongation of shortened AERP at 3 mg/kg, iv measured at 20 to 30 mins
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
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