Urotensin-II receptor antagonist-1

Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor) . Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM) [1].

Product Specifications

CAS Number

[1034708-07-0]

UNSPSC

12352005

Target

Cytochrome P450; Opioid Receptor; Sodium Channel; Urotensin Receptor

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Smiles

CN(CC(N1[C@@H](CN2CCCC2)[C@@H](C3=CC=CC=C3)CCC1)=O)C4=CC=C(Cl)C(Cl)=C4

Molecular Formula

C25H31Cl2N3O

Molecular Weight

460.44

References & Citations

[1]McAtee JJ, et al. Development of potent and selective small-molecule human Urotensin-II antagonists. Bioorg Med Chem Lett. 2008 Jun 15;18 (12) :3500-3.