1034708-07-0
Chemical Structure
Urotensin-II receptor antagonist-1
- CAS No.: 1034708-07-0
- Formula:C25H31Cl2N3O
- Molecular Weight:460.44
IUPAC Name: 2-((3,4-dichlorophenyl)(methyl)amino)-1-((2R,3R)-3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl)ethanone
InChIKey: HXWCQEQIPYCSAM-QPPBQGQZSA-N
SMILES: CN(CC(N1[C@@H](CN2CCCC2)[C@@H](C3=CC=CC=C3)CCC1)=O)C4=CC=C(Cl)C(Cl)=C4
Biological Activity: 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].
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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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