Urotensin-II receptor antagonist-1
Product Specifications
CAS Number
1034708-07-0
Target
GPCR, Cytochromes P450, Opioid Receptor, Sodium Channel
Related Pathways
Endocrinology/Hormones, Metabolism, Neuroscience, Membrane transporter/Ion channel, GPCR/G Protein
Bioactivity
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) .
Smiles
C([C@H]1[C@H](CCCN1C(CN(C)C2=CC(Cl)=C(Cl)C=C2)=O)C3=CC=CC=C3)N4CCCC4
Molecular Formula
C25H31Cl2N3O
Molecular Weight
460.439
Shipping Conditions
Ice Packs
Storage Temperature
-20°C
Available Sizes
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