1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  2. Opioid Receptor Urotensin Receptor Sodium Channel Cytochrome P450
  3. 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).

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Urotensin-II receptor antagonist-1 Chemical Structure

Urotensin-II receptor antagonist-1 Chemical Structure

CAS No. : 1034708-07-0

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Description

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].

IC50 & Target

Urotensin II, κ-Opioid Receptor[1]

Molecular Weight

460.44

Formula

C25H31Cl2N3O

CAS No.
SMILES

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

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Urotensin-II receptor antagonist-1
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HY-10672
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