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Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
Assay data:17 Active, 1 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
Assay data:15 Active, 14 Activity ≤ 1 µM, 17 Tested
Cmax in Rattus norvegicus (rat) at 2 mg/kg, po
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µM
Cmax in Rattus norvegicus (rat) assessed as (S)-3-(1-(benzo[d][1,3]dioxol-5-yl)-2-(2-methoxy-4-methylphenylsulfonamido)-2-oxoethyl)-1-methyl-1H-indole-6-carboxylic acid level at 2 mg/kg, po
Antagonist activity at ETA receptor in Homo sapiens (human) umbilical artery
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Antagonist activity at ETA receptor in Rattus norvegicus (rat) aorta assessed as inhibition of Kcl-induced contraction
Antagonist activity at ETB receptor in Oryctolagus cuniculus (rabbit) pulmonary artery
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Prodrug conversion in Rattus norvegicus (rat) assessed as (S)-3-(1-(benzo[d][1,3]dioxol-5-yl)-2-(2-methoxy-4-methylphenylsulfonamido)-2-oxoethyl)-1-methyl-1H-indole-6-carboxylic acid level at 2 mg/kg, iv
SummaryCompounds, Active
Prodrug conversion in Rattus norvegicus (rat) assessed as (S)-3-(1-(benzo[d][1,3]dioxol-5-yl)-2-(2-methoxy-4-methylphenylsulfonamido)-2-oxoethyl)-1-methyl-1H-indole-6-carboxylic acid level at 2 mg/kg, po
Prodrug conversion in male Rattus norvegicus (rat) liver cytosol assessed as (S)-3-(1-(benzo[d][1,3]dioxol-5-yl)-2-(2-methoxy-4-methylphenylsulfonamido)-2-oxoethyl)-1-methyl-1H-indole-6-carboxylic acid formation
Prodrug conversion in Homo sapiens (human) liver cytosol assessed as (S)-3-(1-(benzo[d][1,3]dioxol-5-yl)-2-(2-methoxy-4-methylphenylsulfonamido)-2-oxoethyl)-1-methyl-1H-indole-6-carboxylic acid formation
Prodrug conversion in Sus scrofa (pig) liver cytosol assessed as (S)-3-(1-(benzo[d][1,3]dioxol-5-yl)-2-(2-methoxy-4-methylphenylsulfonamido)-2-oxoethyl)-1-methyl-1H-indole-6-carboxylic acid formation
Antagonist activity at ETA receptor in Rattus norvegicus (rat) assessed as inhibition of ET1-induced pressor response at 0.1 mg/kg, po administered 3 hr post ET1-induction
Antagonist activity at ETA receptor in Rattus norvegicus (rat) assessed as inhibition of ET1-induced pressor response at 0.6 mg/kg, po administered 3 hr post ET1-induction
Antagonist activity at ETA receptor in Rattus norvegicus (rat) assessed as inhibition of ET1-induced pressor response at 10 mg/kg, po administered 3 hr post ET1-induction measured up to 12 hr
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