SML3013
LY2886721
≥98% (HPLC)
别名:
LY 2886721, LY-2886721, N-(3-((4aS,7aS)-2-Amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide, N-[3-[(4aS ,7aS )-2-Amino-4a,5-dihydro-4H-furo[3,4-d ][1,3]thiazin-7a(7H )-yl]-4-fluorophenyl]-5-fluoro-2-pyridinecarboxamide
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选择尺寸
关于此项目
经验公式（希尔记法）:
C18H16F2N4O2S
化学文摘社编号:
分子量:
390.41
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
LY2886721, ≥98% (HPLC)
InChI
1S/C18H16F2N4O2S/c19-11-1-4-15(22-6-11)16(25)23-12-2-3-14(20)13(5-12)18-9-26-7-10(18)8-27-17(21)24-18/h1-6,10H,7-9H2,(H2,21,24)(H,23,25)/t10-,18-/m0/s1
SMILES string
FC1=CC=C(NC(C2=CC=C(C=N2)F)=O)C=C1[C@@]34[C@@](CSC(N)=N4)([H])COC3
InChI key
NIDRNVHMMDAAIK-YPMLDQLKSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Orally active, potent and selective β-secretase (BACE) active site inhibitor with amyloid β-lowering efficacy in cultures and in animal models in vivo.
Y2886721 is an orally active, potent and selective β-secretase (BACE) active site inhibitor (human BACE1/2 IC50 = 20.3/10.2 nM; cathepsin D/pepsin/renin IC50 >10 μM). Y2886721 exhibits amyloid β-lowering efficacy in cultures (Aβ1-40/Aβ1-42 IC50 = 18.5/19.7 nM with APP751 Swedish mutation-expressing HEK293 and 10.7/9.2 nM with primary cortical neurons from PDAPP transgenic mouse embryos) and in animal models in vivo (3-30 mg/kg PDAPP mice, 1.5 mg/kg beagle dogs; p.o.).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Ling Li et al.
Cell proliferation, 53(4), e12798-e12798 (2020-03-28)
Alzheimer's disease (AD) is the most common neurodegenerative disease which is characterized by the formation of amyloid beta (Aβ) plaques and neurofibrillary tangles. These abnormal proteins induce disturbance in mitochondrial dynamics and defect in autophagy system. Since presenilin-1 (PS1) is
Akihiro Takano et al.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 60(7), 992-997 (2018-12-12)
β-secretase 1 (BACE1) is a key enzyme in the generation of β-amyloid, which is accumulated in the brain of Alzheimer disease patients. PF-06684511 was identified as a candidate PET ligand for imaging BACE1 in the brain and showed high specific
Tugce Munise Satir et al.
Alzheimer's research & therapy, 12(1), 63-63 (2020-05-28)
Alzheimer's disease (AD) is the most common form of age-related neurodegenerative diseases. Cerebral deposition of Aβ peptides, especially Aβ42, is considered the major neuropathological hallmark of AD and the putative cause of AD-related neurotoxicity. Aβ peptides are produced by sequential
Patrick C May et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 35(3), 1199-1210 (2015-01-23)
BACE1 is a key protease controlling the formation of amyloid β, a peptide hypothesized to play a significant role in the pathogenesis of Alzheimer's disease (AD). Therefore, the development of potent and selective inhibitors of BACE1 has been a focus
Lu Zhao et al.
Cells, 8(5) (2019-05-22)
β-site APP-cleaving enzyme 1 (BACE1) initiates amyloid precursor protein (APP) cleavage and β-amyloid (Aβ) production, a critical step in the pathogenesis of Alzheimer's disease (AD). It is thus of considerable interest to investigate how BACE1 activity is regulated. BACE1 has
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