Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, K i =16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 ( IC 50 =0.75 μM, CYP2D6 ; 1.4 μM, CYP3A4 ), inhibits κ-opioid receptor ( EC 50 =3.2 μM), targets cardiac sodium channels (K i =2.5 μM).
Products | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Signaling Pathways > GPCR/G Protein | Products > Signaling Pathways > Neuronal Signaling | Products > Signaling Pathways > Membrane Transporter/Ion Channel | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Cardiovascular Disease | Products > Signaling Pathways > Urotensin Receptor | Products > Signaling Pathways > Opioid Receptor | Products > Signaling Pathways > Sodium Channel | Products > Signaling Pathways > Cytochrome P450
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