Urotensin-II receptor antagonist-1 - CAS 1034708-07-0

Urotensin-II receptor antagonist-1 (compound 1) is a human Urotensin II receptor antagonist with low oral bioavailability (F=0-3% in rats) and a Ki of 16 nM in HEK293 cells expressing human recombinant UT receptors. It inhibits cytochrome P450 enzymes (IC50=0.75 μM for CYP2D6; 1.4 μM for CYP3A4), suppresses κ opioid receptors (EC50=3.2 μM), and targets cardiac sodium channels (Ki=2.5 μM) .

GPCR, Cytochromes P450, Opioid Receptor, Sodium Channel

Endocrinology/Hormones, Metabolism, Neuroscience, Membrane transporter/Ion channel, GPCR/G Protein

1034708-07-0

C25H31Cl2N3O

460.439

C([C@H]1[C@H](CCCN1C(CN(C)C2=CC(Cl)=C(Cl)C=C2)=O)C3=CC=CC=C3)N4CCCC4

-20°C

Ice Packs

Small Compound