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TAK-070

Names

[ CAS No. ]:
365276-12-6

[ Name ]:
TAK-070

[Synonym ]:
2-[(2R)-6-(4-Biphenylylmethoxy)-1,2,3,4-tetrahydro-2-naphthalenyl]-N,N-dimethylethanamine hydrochloride hydrate
EAC604ZY07
2-Naphthaleneethanamine, 6-([1,1'-biphenyl]-4-ylmethoxy)-1,2,3,4-tetrahydro-N,N-dimethyl-, (2R)-, hydrochloride, hydrate (1:1:1)
TAK-070

Biological Activity

[Description]:

A selective, nonpeptidic, noncompetitive BACE1 inhibitor with IC50 of 3.15 uM in cell-free assays; suppresses the secretion of Aβ with minimum effective concentrations (MECs) for Aβ40 and Aβ42 of 100 and 1000 nM respectively in human IMR-32 neuroblastoma cells, also stimulates sAPPα production with MEC of 100 nM, significantly decreases the secreted level of both human Swedish sAPPβ and mouse endogenous sAPPβ, N-terminal counterparts of APP generated by BACE1 cleavage, by ∼16 and ∼19% respectively at 3 uM; ameliorates Abeta pathology and behavioral deficits in a mouse model of Alzheimer's disease.

[References]

References 1. Fukumoto H, et al. J Neurosci. 2010 Aug 18;30(33):11157-66. 2. Takahashi H, et al. Brain Res. 2010 Nov 18;1361:146-56. View Related Products by Target Beta-secretase (BACE)

Chemical & Physical Properties

[ Molecular Formula ]:
C27H31NO.HCl.H2O

[ Molecular Weight ]:
440.017

[ Exact Mass ]:
439.227814

Related Compounds