Identification | Back Directory | [Name]
Ethanone, 1-[4-[2-[[1-(3,4-difluorophenyl)-1H-pyrazol-3-yl]methoxy]ethyl]-1-piperazinyl]- | [CAS]
1351438-26-0 | [Synonyms]
Ethanone, 1-[4-[2-[[1-(3,4-difluorophenyl)-1H-pyrazol-3-yl]methoxy]ethyl]-1-piperazinyl]- | [Molecular Formula]
C18H22F2N4O2 | [MOL File]
1351438-26-0.mol | [Molecular Weight]
364.39 |
Hazard Information | Back Directory | [Description]
EST64454 is a σ1 receptor (σ1R) antagonist clinical candidate for the treatment of pain. EST64454 shows an outstanding aqueous solubility, which together with its high permeability in Caco-2 cells will allow its classification as a BCS class I compound. It also shows high metabolic stability. | [Uses]
EST64454 (compound 9k) is a selective, orally active sigma-1 receptor antagonist with Ki 22 nM. EST64454 can be used to study pain[1]. | [IC 50]
σ1R: 22 nM (Ki) | [References]
[1] Yeste S, et al. Preliminary in Vitro Assessment of the Potential of EST64454, a Sigma-1 Receptor Antagonist, for Pharmacokinetic Drug-Drug Interactions. Biol Pharm Bull. 2020;43(1):68-76. DOI:10.1248/bpb.b19-00542 |
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