| Identification | Back Directory | [Name]
Ethanone, 2-[(3,4-dichlorophenyl)MethylaMino]-1-[(2R,3R)-3-phenyl-2-(1-pyrrolidinylMethyl)-1-piperidinyl]-, rel- | [CAS]
1034708-07-0 | [Synonyms]
2-(3,4-dichloro-N-methylanilino)-1-[(2S,3S)-3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethanone
Ethanone, 2-[(3,4-dichlorophenyl)MethylaMino]-1-[(2R,3R)-3-phenyl-2-(1-pyrrolidinylMethyl)-1-piperidinyl]-, rel- | [Molecular Formula]
C25H31Cl2N3O | [MOL File]
1034708-07-0.mol | [Molecular Weight]
460.44 |
| Hazard Information | Back Directory | [Uses]
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]. | [References]
[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. DOI:10.1016/j.bmcl.2008.05.027 |
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